Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
869 Cards in this Set
- Front
- Back
Basic Pharmacokinetics
|
...
|
|
Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
|
Half-life (T1/2)
|
|
Relates the amount of drug in the body to the plasma concentration
|
Volume of distribution (VD)
|
|
Plasma concentration of a drug at a given time
|
Cp
|
|
The ratio of the rate of elimination of a drug to its plasma concentration
|
Clearance (CL)
|
|
The elimination of drug that occurs before it reaches the systemic circulation
|
First pass effect
|
|
The fraction of administered dose of a drug that reaches systemic circulation
|
Bioavailability (F)
|
|
When the rate of drug input equals the rate of drug elimination
|
Steady state
|
|
Metabolism
|
...
|
|
This step of metabolism makes a drug more hydrophilic and hence augments elimination
|
Phase I
|
|
Different steps of Phase I
|
Oxidation, reduction, hydrolysis
|
|
Inducers of Cytochrome P450 (CYP450)
|
Barbiturates, phenytoin, carbamazepine, rifampin, St. John's Wort
|
|
Inhibitors of CYP450
|
Amiodarone, Diltiazem, Verapamil, Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
|
|
Products of Phase II conjugation
|
Glucuronate, acetic acid, and glutathione sulfate
|
|
Type of kinetics when a constant percentage of substrate is metabolized per unit time
|
First order kinetics
|
|
Drug elimination with a constant amount metabolized regardless of drug concentration
|
Zero order kinetics
|
|
Target plasma concentration times (volume of distribution divided by bioavailability)
|
Loading dose (Cp*(Vd/F))
|
|
Concentration in the plasma times (clearance divided by bioavailability)
|
Maintenance dose (Cp*(CL/F))
|
|
Pharmacodynamics
|
...
|
|
Strength of interaction between drug and its receptor
|
Affinity
|
|
Selectivity of a drug for its receptor
|
Specificity
|
|
Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
|
Potency
|
|
Maximum response achieveable from a drug
|
Efficacy
|
|
Ability of a drug to produce 100% of the maximum response regardless of the potency
|
Full agonist
|
|
Ability to produce less than 100% of the response
|
Partial agonist
|
|
Ability to bind reversibly to the same site as the drug and without activating the effector system
|
Competitive antagonist
|
|
Class of drugs with ability to decrease the maximal response to an agonist
|
Noncompetitive antagonist
|
|
A hormone whose mechanism of action (MOA) utilizes intracellular receptors
|
Thyroid and steroid hormones
|
|
A hormone whose MOA utilizes transmembrane receptors
|
Insulin
|
|
Class of drugs whose MOA utilizes ligand gated ion channels
|
Benzodiazepines and calcium channel blockers
|
|
Median effective dose required for an effect in 50% of the population
|
ED50
|
|
Median toxic dose required for a toxic effect in 50% of the population
|
TD50
|
|
Dose which is lethal to 50% of the population
|
LD50
|
|
Window between therapeutic effect and toxic effect
|
Therapeutic index
|
|
Term for a high margin of safety
|
High therapeutic index
|
|
Term for a narrow margin of safety
|
Low therapeutic index
|
|
Antidotes and agents used in drug overdose
|
...
|
|
Antidote used for lead poisoning
|
Dimercaprol, EDTA
|
|
Antidote used for cyanide poisoning
|
Nitrites
|
|
Antidote used for anticholinergic poisoning
|
Physostigmine
|
|
Antidote used for organophosphate/anticholinesterase poisoning
|
Atropine, pralidoxime (2-PAM)
|
|
Antidote used for iron salt toxicity
|
Deferoxamine
|
|
Antidote used for acetaminophen (APAP) toxicity
|
N-acetylcysteine (Mucomyst)
|
|
Antidote for arsenic, mercury, lead, and gold poisoning
|
Dimercaprol
|
|
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
|
Penicillamine
|
|
Antidote used for heparin overdose
|
Protamine
|
|
Antidote used for warfarin toxicity
|
Vitamin K and Fresh frozen plasma (FFP)
|
|
Antidote for tissue plasminogen activator (t-PA), streptokinase
|
Aminocaproic acid
|
|
Antidote used for methanol and ethylene glycol
|
Ethanol or fomepizole
|
|
Antidote used for opioid toxicity
|
Naloxone (IV), naltrexone (PO)
|
|
Antidote used for benzodiazepine toxicity
|
Flumazenil
|
|
Antidote used for tricyclic antidepressants (TCA)
|
Sodium bicarbonate
|
|
Antidote used for carbon monoxide poisoning
|
100% O2 and hyperbaric O2
|
|
Antidote used for digitalis toxicity
|
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
|
|
Antidote used for beta agonist toxicity (eg. Metaproterenol)
|
Esmolol
|
|
Antidote for methotrexate toxicity
|
Leucovorin
|
|
Antidote for beta-blockers and hypoglycemia
|
Glucagon
|
|
Antidote useful for some drug induced Torsade de pointes
|
Magnesium sulfate
|
|
Antidote for hyperkalemia
|
sodium polystyrene sulfonate (Kayexalate)
|
|
Antidote for salicylate intoxication
|
Alkalinize urine, dialysis
|
|
Cancer Chemotherapy
|
...
|
|
Relationship of tumor cell number to time of diagnosis, symptoms, treatment and survival
|
Log-kill hypothesis
|
|
Pyrimidine analog that causes "thymineless death" given with leucovorin rescue
|
5-fluorouracil (5-FU)
|
|
Drug used in cancer therapy causes Cushing-like symptoms
|
Prednisone
|
|
Side effect of Mitomycin
|
SEVERE myelosuppression
|
|
MOA of cisplatin
|
Alkylating agent
|
|
Common toxicities of cisplatin
|
Nephro and ototoxicity, peripheral neuropathy
|
|
Analog of hypoxanthine, needs HGPRTase for activation
|
6-mercaptopurine (6-MP)
|
|
Interaction with this drug requires dose reduction of 6-MP
|
Allopurinol
|
|
Iron-chelating agent, protects against doxorubicin toxicity by scavenging free radicals
|
Dexrazoxane
|
|
Blows DNA (breaks DNA strands), limiting SE is pulmonary toxicity
|
Bleomycin
|
|
Platinum-based combination therapy for testicular cancer
|
Bleomycin+etoposide+cisplatin
|
|
ABVD regimen used for Hodgkin's, but appears less likely to cause sterility and secondary malignancies than MOPP
|
Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
|
|
Regimen used for non-Hodgkin's lymphoma
|
CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
|
|
Regimen used for breast cancer
|
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
|
|
Alkylating agent, vesicant that causes tissue damage with extravasation
|
Mechlorethamine
|
|
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
|
Cyclophosphamide
|
|
Microtubule inhibitor that causes peripheral sensory neuropathy, foot drop (eg. ataxia), and SIADH
|
Vincristine
|
|
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
|
Paclitaxel (taxol)
|
|
Agent similar to cisplatin, less nephrotoxic, greater myelosuppression, used to treat refractory hematologic malignancies
|
Carboplatin
|
|
Anti-androgen used for prostate cancer
|
Flutamide, bicalutamide, nilutamide
|
|
Anti-estrogen used for estrogen receptor + breast cancer
|
Tamoxifen
|
|
Aromatase inhibitor used in breast cancer
|
anastrozole
|
|
Newer biologic agent approved for metastatic melanoma, enhances T-cell immune responses
|
Ipilimumab
|
|
Some cell cycle specific anti-cancer drugs
|
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
|
|
Some cell cycle non-specific drugs
|
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin
|
|
Regimen used for advanced colorectal cancer, stage II and III colon cancer
|
FOLFOX (oxaliplatin, 5-FU and leucovorin)
|
|
Nitrosoureas with high lipophilicity, used for brain tumors
|
lomustine
|
|
Anti-cancer agents that affect the VEGF-signaling pathway
|
Bevacizumab, Ziv-aflibercept, Sorafenib, Sunitinib, Pazopanib
|
|
Endocrine drugs: hypothalamic and pituitary hormones
|
...
|
|
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
|
Octreotide
|
|
Somatotropin (GH) analog used in GH deficiency (dwarfism)
|
Somatrem
|
|
GHRH analog used as diagnostic agent
|
Sermorelin
|
|
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
|
Leuprolide
|
|
GnRH antagonist with more immediate effects, used for infertility
|
Ganirelix
|
|
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
|
Bromocriptine
|
|
Hormone inhibiting prolactin release
|
Dopamine
|
|
ACTH analog used for diagnosis of patients with corticosteroid abnormality
|
Cosyntropin
|
|
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
|
Desmopressin (DDAVP)
|
|
SE of OCs
|
Increased thromboembolic events
|
|
Thyroid and anti-thyroid drugs
|
...
|
|
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
|
L-thyroxine (T4)
|
|
T3 compound less widely used
|
Cytomel
|
|
Anti-thyroid drugs
|
Thioamides, iodides, radioactive iodine, and ipodate
|
|
Thioamide agents used in hyperthyroidism
|
Methimazole and propylthiouracil (PTU)
|
|
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
|
PTU
|
|
PTU (propylthiouracil) MOA
|
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
|
|
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
|
Iodide salts
|
|
Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
|
Thyroxine
|
|
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
|
Radioactive iodine
|
|
Radio contrast media that inhibits the conversion of T4 to T3
|
Ipodate
|
|
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
|
Beta-blockers such as propranolol
|
|
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
|
Iron deiodinates thyroxine
|
|
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
|
Estogens increase maternal TBG
|
|
Adrenocorticosteroid and adrenocortical antagonists
|
...
|
|
3 zones of adrenal cortex and their products
|
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
|
|
Mnemonic for 3 zones of adrenal cortex
|
GFR
|
|
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
|
Glucocorticoids
|
|
Short-medium acting glucocorticoids
|
Cortisone, Hydrocortisone, Prednisone, Prednisolone, Methylprednisolone
|
|
Intermediate acting glucocorticoids
|
Triamcinolone, Fluprednisolone
|
|
Long acting glucocorticoids
|
Betamethasone and dexamethasone
|
|
Mineralocorticoids
|
Fludrocortisone and deoxycorticosterone
|
|
Some side effects of corticosteroids
|
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
|
|
Inhibitors of corticosteroids biosynthesis
|
...
|
|
Used for Cushing's syndrome (increased corticosteroid)
|
Dexamethasone suppression test
|
|
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
|
Aminoglutethimide
|
|
Antifungal agent used for inhibition of all gonadal and adrenal steroids
|
Ketoconazole
|
|
Antiprogestin used as potent antagonist of GC receptor
|
Mifepristone
|
|
Diuretic used to antagonize aldosterone receptors
|
Spironolactone
|
|
Common SE of spironolactone
|
Gynecomastia and hyperkalemia
|
|
Gonadal hormones and inhibitors
|
...
|
|
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
|
Estrogen
|
|
Antiestrogen drugs used for fertility and breast cancer respectively
|
Clomiphene and tamoxifen
|
|
Common SE of tamoxifen and raloxifene
|
Hot flashes
|
|
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
|
Raloxifene
|
|
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
|
Diethylstilbestrol (DES)
|
|
Estrogen mostly used in oral contraceptives (OC)
|
Ethinyl estradiol and mestranol
|
|
Anti-progesterone used as abortifacient
|
Mifepristone (RU-486)
|
|
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
|
Combination oral contraceptives (OC)
|
|
Oral contraceptive available in a transdermal patch
|
Ortho-Evra
|
|
Converted to more active form DHT by 5 alpha-reductase
|
Testosterone
|
|
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
|
Finasteride (Proscar and Propecia respectively)
|
|
Anabolic steroid that has potential for abuse
|
Nandrolone, oxymetholone, and oxandrolone
|
|
Anti-androgen used for hirsutism in females
|
Cyproterone acetate
|
|
Drug is used with testosterone for male fertility
|
Leuprolide
|
|
Pancreatic hormones, antidiabetics, and hyperglycemics
|
...
|
|
What do alpha cells in the pancreas produce?
|
Glucagon
|
|
What do beta cells in the pancreas produce?
|
Insulin
|
|
Where are beta cells found in the pancreas?
|
Islets of Langerhans
|
|
What do delta cells in the pancreas produce?
|
Somatostatin
|
|
Product of proinsulin cleavage used to assess insulin production
|
C-peptide
|
|
Exogenous insulin contains
|
No C-peptide
|
|
Endogenous insulin contains
|
Normal C-peptide
|
|
Very rapid acting insulin, having fastest onset and shortest duration of action
|
Lispro (Humalog), aspart (Novolog), glulisine (Apidra)
|
|
Short acting, crystalline zinc insulin used to reverse acute hyperglycemia
|
Regular (Humulin/Novolin R)
|
|
Long acting insulins
|
Glargine, detemir
|
|
Major SE of insulin
|
Hypoglycemia
|
|
Important in synthesis of glucose to glycogen in the liver
|
GLUT 2
|
|
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
|
GLUT 4
|
|
Examples of alpha-glucosidase inhibitors (AGI)
|
Acarbose, miglitol
|
|
MOA of AGI's
|
Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides
|
|
SE of AGI's
|
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
|
|
Alpha-glucosidase inhibitor associated with elevation of LFT's
|
Acarbose
|
|
Amino acid derivative, active as an insulin secretagogue
|
Nateglinide
|
|
MOA of nateglinide
|
Insulin secretagogue - closes ATP-sensitive K+ channel
|
|
Biguanide
|
Metformin
|
|
Drugs available in combination with metformin
|
Glyburide, glipizide, sitagliptin, saxagliptin, pioglitazone
|
|
MOA of metformin
|
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
|
|
Vascular effects of metformin
|
Decreased micro and macro vascular disease
|
|
Most important potential SE of metformin
|
Lactic acidosis
|
|
Incidence of hyoglycemia with metformin
|
None
|
|
Meglitinide class of drugs
|
Repaglinide
|
|
MOA of repaglinide
|
Insulin release from pancreas; faster and shorter acting than sulfonylurea
|
|
First generation sulfonylurea
|
Chlorpropamide, tolbutamide, tolazamide, etc.
|
|
Second generation sulfonylurea
|
Glyburide, glipizide, glimepiride, etc.
|
|
MOA of both generations
|
Insulin release from pancreas by modifying K+ channels
|
|
Common SE of sulfonylureas, repaglinide, and nateglinide
|
Hypoglycemia, weight gain
|
|
Sulfonylurea NOT recommended for elderly because of very long half life
|
Chlorpropamide
|
|
Thiazolidinediones
|
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
|
|
Reason troglitazone was withdrawn from market
|
Hepatic toxicity
|
|
MOA of thiazolidinediones
|
Decrease insulin resistance, stimulate PPAR-gamma receptors
|
|
SE of Thiazolindinediones
|
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism, risk for angina/MI
|
|
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
|
Glucagon
|
|
Drugs used in bone homeostasis
|
...
|
|
Available bisphosphonates
|
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
|
|
MOA of Bisphosphonates
|
Inhibits osteoclast bone resorption
|
|
Names of three bisphosphonates available IV
|
Pamidronate, zoledronate, ibandronate
|
|
Uses of bisphosphonates
|
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
|
|
Major SE of bisphosphonates
|
Chemical esophagitis
|
|
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
|
Etidronate
|
|
Used for prevention of postmenopausal osteoporosis in women
|
Estrogen (HRT-Hormone replacement therapy)
|
|
Increase bone density, also being tested for breast CA prophylaxis
|
Raloxifene (SERM-selective estrogen receptor modulator)
|
|
Used intranasally and decreases bone resorption
|
Calcitonin (salmon prep)
|
|
Used especially in postmenopausal women, dosage should be 1500 mg
|
Calcium
|
|
Vitamin given with calcium to ensure proper absorption
|
Vitamin D
|
|
Drugs with important actions on smooth muscle
|
...
|
|
Disease caused by excess ergot alkaloids
|
St. Anthony's Fire
|
|
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
|
Autocoids
|
|
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
|
Zollinger-Ellison Syndrome
|
|
Drug that causes contraction of the uterus
|
Oxytocin
|
|
Distribution of histamine receptors H1, H2, and H3
|
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
|
|
Prototype antagonist of H1 and H2 receptors
|
Diphenhydramine and cimetidine, respectively
|
|
1st generation antihistamine that is highly sedating
|
Diphendydramine
|
|
1st generation antihistamine that is least sedating
|
Chlorpheniramine or cyclizine
|
|
2nd generation antihistamines
|
Fexofenadine, loratadine, and cetirizine
|
|
Generation of antihistamine that has the most CNS effects
|
First generation due to being more lipid-soluble
|
|
Major indication for H1 receptor antagonist
|
Use in IgE mediated allergic reaction
|
|
Antihistamine that can be used for anxiety and insomnia and is not addictive
|
hydroxyzine (Atarax)
|
|
H1 antagonist used in motion sickness
|
Dimenhydrinate, meclizine, and other 1st generation
|
|
Most common side effect of 1st generation antihistamines
|
Sedation
|
|
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
|
Terfenadine and astemizole (have been removed from the market)
|
|
H2 blocker that causes the most interactions with other drugs
|
Cimetidine
|
|
Clinical use for H2 blockers
|
Acid reflux disease, duodenal ulcer and peptic ulcer disease
|
|
Receptors for serotonin (5HT-1) are located
|
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
|
|
"
|
...
|
|
5HT-1d agonist used for migraine headaches "
|
Sumatriptan, naratriptan, and rizatriptan
|
|
Triptan available in parenteral and nasal formulation
|
Sumatriptan
|
|
H1 blocker that is also a serotonin antagonist
|
Cyproheptadine
|
|
Agents for reduction of postpartum bleeding
|
Oxytocin, ergonovine and ergotamine
|
|
Agents used in treatment of carcinoid tumor
|
Ketanserin cyproheptadine, and phenoxybenzamine
|
|
5HT-3 antagonist used in chemotherapeutic induced emesis
|
"Ondansetron, granisetron,
|
|
dolasetron and alosetron "
|
...
|
|
5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
|
Dolasetron
|
|
DOC to treat chemo-induced nausea and vomiting
|
Odansetron
|
|
Drug used in ergot alkaloids overdose, ischemia and gangrene
|
Nitroprusside
|
|
Reason ergot alkaloids are contraindicated in pregnancy
|
Uterine contractions
|
|
SE of ergot alkaloids
|
Hallucinations resembling psychosis
|
|
Ergot alkaloid used as an illicit drug
|
LSD
|
|
Dopamine agonist used in hyperprolactinemia
|
Bromocriptine
|
|
Peptide causing increased capillary permeability and edema
|
Bradykinin and histamine
|
|
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
|
Bradykinin
|
|
Drug causing depletion of substance P (vasodilator)
|
Capsaicin
|
|
Prostaglandins that cause abortions
|
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
|
|
"
|
...
|
|
Difference between COX 1 and COX 2 "
|
"COX 1 is found throughout
|
|
the body and COX 2 is only
|
...
|
|
in inflammatory tissue"
|
...
|
|
Drug that selectively inhibits COX 2
|
Celecoxib and rofecoxib
|
|
Inhibitor of lipoxygenase
|
Zileuton
|
|
Major SE of zileuton
|
Liver toxicity
|
|
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
|
Zafirlukast and montelukast
|
|
Used in pediatrics to maintain patency of ductus arteriosis
|
PGE1
|
|
Approved for use in severe pulmonary HTN
|
PGI2 (epoprostenol)
|
|
Prostaglandin used in the treatment of impotence
|
Alprostadil
|
|
Irreversible, nonselective COX inhibitor
|
Aspirin
|
|
Class of drugs that reversibly inhibit COX
|
NSAIDS
|
|
Primary endogenous substrate for Nitric Oxidase Synthase
|
Arginine
|
|
MOA and effect of nitric oxide
|
Stimulates cGMP which leads to vascular smooth muscle relaxation
|
|
Long acting beta 2 agonist used in asthma
|
Salmeterol, formoterol
|
|
Muscarinic antagonist used in asthma
|
Ipratropium
|
|
MOA action of cromolyn
|
Mast cell stabilizer
|
|
Methylxanthine derivative used as a remedy for intermittent claudication
|
Pentoxifylline
|
|
"
|
...
|
|
MOA of corticosteroids"
|
inhibit phospholipase A2
|
|
SE of long term corticosteroid therapy and remedy
|
Adrenal suppression and weaning slowly, respectively
|
|
Antimicrobials
|
...
|
|
MOA of quinolones
|
Inhibit DNA gyrase
|
|
MOA of penicillin
|
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
|
|
Drug used for MRSA
|
Vancomycin
|
|
Vancomycin MOA
|
Blocks cell wall synthesis by sequestration
|
|
Genetic basis of low level resistance found with vancomycin
|
Point mutation
|
|
Meningitis prophylaxis for persons in contact with patients
|
Ciprofloxacin or Rifampin (for children less than 4 yrs old)
|
|
Technique used to diagnose perianal itching, and the drug used to treat it
|
"Scotch tape technique
|
|
and mebendazole"
|
...
|
|
Two toxicities of aminoglycosides
|
nephro and ototoxicity
|
|
DOC for Legionnaires' disease
|
Moxifloxacin
|
|
MOA of sulfonamides
|
Inhibit dihydropteroate synthase
|
|
Penicillins active against penicillinase secreting bacteria
|
Methicillin, nafcillin, and dicloxacillin
|
|
Cheap wide spectrum antibiotic DOC for otitis media
|
Amoxicillin
|
|
Class of antibiotics that have 10% cross sensitivity with penicillins
|
Cephalosporins
|
|
PCN active against pseudomonas
|
ceftazidime, imipenem, piperacillin and ticarcillin
|
|
Antibiotic causing red-man syndrome, and prevention
|
"Vancomycin, infusion
|
|
at a slow rate and antihistamines"
|
...
|
|
Drug causes teeth discoloration
|
Tetracycline
|
|
MOA of tetracycline
|
Decreases protein synthesis by inhibiting 30S ribosome
|
|
Drug that causes gray baby syndrome and aplastic anemia
|
Chloramphenicol
|
|
Drug notorious for causing pseudomembranous colitis
|
Clindamycin, metronidazole
|
|
DOC for tx of pseudomembranous colitis (mild)
|
Metronidazole
|
|
Treatment of severe/relapsing pseudomembranous colitis
|
ORAL vancomycin
|
|
Anemia caused by trimethoprim
|
Megaloblastic anemia
|
|
Reason fluoroquinolones are contraindicated in children and pregnancy
|
Cartilage damage
|
|
DOC for giardia, bacterial vaginosis, and trichomonas
|
Metronidazole
|
|
Treatment for TB patients (think RIPE)
|
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
|
|
Metronidazole SE if given with alcohol
|
Disulfiram-like reaction
|
|
Common side effect of Rifampin
|
Red urine discoloration
|
|
MOA of nystatin
|
Bind ergosterol in fungal cell membrane
|
|
Neurotoxicity with isoniazid (INH) prevented by
|
Administration of Vit. B6 (pyridoxine)
|
|
Toxicity of amphotericin
|
Nephrotoxicity
|
|
SE seen only in men with administration of ketoconazole
|
Gynecomastia
|
|
Topical DOC in impetigo
|
Topical mupirocin (Bactroban)
|
|
Drug used for African sleeping sickness
|
Suramin
|
|
Drug used in Chagas disease
|
Nifurtimox
|
|
Cephalosporins able to cross the BBB
|
Ceftazidime, Ceftriaxone or Cefotaxime
|
|
Oral 3rd generation cephalosporins NOT able to cross the BBB
|
Cefixime
|
|
Drug used for N. gonorrhea in females
|
Ceftriaxone
|
|
Cephalosporin causes kernicterus in neonates
|
Ceftriaxone or cefuroxime
|
|
SE of INH
|
Peripheral neuritis and hepatitis
|
|
Aminoglycoside that is least ototoxic
|
Streptomycin
|
|
Drug used in exoerythrocytic cycle of malaria
|
Primaquine
|
|
Oral antibiotic of choice for moderate inflammatory acne
|
Minocycline
|
|
Drug of choice for leprosy
|
Dapsone, rifampin and clofazimine combination
|
|
DOC for herpes and its MOA
|
Acyclovir; phosphorylation, incorporation into viral DNA, and chain termination
|
|
Anti-bacterials that cause hemolysis in G6PD-deficient patients
|
Sulfonamides
|
|
MOA of erythromycin
|
Inhibition of protein synthesis at the 50s subunit of ribosome
|
|
Anti-biotic frequently used for chronic UTI prophylaxis
|
sulfamethoxazole/ trimethoprim
|
|
Lactams that can be used in PCN allergic patients
|
Aztreonam/carbapenems
|
|
SE of imipenem
|
Seizures
|
|
Antiviral Agents
|
...
|
|
DOC for influenza A
|
Oseltamivir
|
|
DOC for severe RSV
|
Ribavirin
|
|
DOC for CMV retinitis
|
Ganciclovir, valganciclovir
|
|
SE for ganciclovir
|
myelosuppression
|
|
Anti-viral agent associated with Stephen Johnson syndrome
|
Nevirapine
|
|
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
|
Protease inhibitors
|
|
Protease inhibitors recommended for pregnant women
|
lopinavir, ritonavir, atazanavir
|
|
Antivirals that are teratogens
|
Delavirdine, efavirenz, and ribavirin
|
|
Single dose used to prevent perinatal transmission of HIV
|
Nevirapine
|
|
Anti-viral with a dose limiting toxicity of pancreatitis
|
Didanosine
|
|
Anti-HSV/VZV agent that causes thrombotic thrombocytopenic purpura/hemolytic uremic syndrome in high doses
|
Valacyclovir
|
|
Intravenous drug effective for end-organ CMV disease (retinitis, colitis, esophagitis)
|
Foscarnet
|
|
Nucleoside reverse transcriptase inhibitor that can cause fatal hypersensitivity reactions linked to HLDB5701
|
Abacavir
|
|
Polymerase inhibitor used to treat Hepatitis C infections in combination with ribavarin
|
Sofosbuvir
|
|
Protease inhibitors used to treat Hepatitis C infections
|
Boceprevir, Simeprevir, Telaprevir
|
|
Sedative Hypnotics
|
...
|
|
Common side effect of hypnotic agents
|
Sedation
|
|
Occurs when sedative hypnotics are used chronically or at high doses
|
Tolerance
|
|
The most common type of drug interaction of sedative hypnotics with other depressant medications
|
Additive CNS depression
|
|
Benzodiazepines used to promote sleep
|
Temazpam, trizolam, flurazepam
|
|
Benzodiazepine used for anxiety
|
Alprazolam
|
|
Non-benzodiazepine used as an anxiolytic
|
Buspirone
|
|
Non-benzodiazepine used for sleep
|
Zolpidem
|
|
Major effect of benzodiazepines on sleep at high doses
|
REM is decreased
|
|
Neurologic SE of benzodiazepines
|
Anterograde amnesia
|
|
Reason benzos are used cautiously in pregnancy
|
Ability to cross the placenta
|
|
Main route of metabolism for benzodiazepines
|
Hepatic
|
|
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
|
Lorazepam, oxazepam, and temazepam
|
|
"MOA for benzodiazepines
|
...
|
|
"
|
increase the FREQUENCY of GABA-mediated chloride ion channel opening
|
|
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
|
Flumazenil
|
|
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
|
Diazepam
|
|
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
|
Clonazepam
|
|
Benzodiazepines that are the most effective in the treatment of panic disorder
|
Alprazolam and Clonazepam
|
|
"Benzodiazepine that is used for anesthesia
|
...
|
|
"
|
Midazolam
|
|
DOC for status epilepticus
|
Diazepam
|
|
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
|
Chlordiazepoxide and Diazepam
|
|
Agents having active metabolites, long half lives, and a high incidence of adverse effects
|
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
|
|
Barbiturates
|
...
|
|
Barbiturates may precipitate this hematologic condition
|
Acute intermittent porphyria
|
|
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
|
Liver enzyme INDUCTION
|
|
Barbiturates MOA
|
Increase the DURATION of GABA-mediated chloride ion channels
|
|
Barbiturate used for the induction of anesthesia
|
Thiopental
|
|
Others
|
...
|
|
Site of action for zaleplon and zolpidem
|
Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
|
|
Good hypnotic activity with less CNS SE than most benzodiazepines
|
Zolpidem, zaleplon
|
|
Agent that is a partial agonist for the 5-HT1A receptor
|
Buspirone
|
|
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
|
Buspirone
|
|
Alcohols
|
...
|
|
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
|
Ethanol
|
|
Agent with zero-order kinetics
|
Ethanol
|
|
Rate limiting step of alcohol metabolism
|
Aldehyde dehydrogenase
|
|
System that increases in activity with chronic ethanol exposure and may contribute to tolerance
|
MEOS
|
|
Enzyme that metabolizes acetaldehyde to acetate
|
Aldehyde dehydrogenase
|
|
Agents that inhibit acetaldehyde dehydrogenase
|
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
|
|
Agent that inhibits alcohol dyhydrogenase and its clinical use
|
FOMEPIZOLE - used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
|
|
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
|
Disulfiram
|
|
The most common neurologic abnormality in chronic alcoholics
|
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
|
|
Agent that is teratogen and causes a fetal syndrome
|
Ethanol
|
|
Agent that is the antidote for methanol overdose
|
Ethanol, fomepizole
|
|
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
|
Fomepizole
|
|
Anti seizure Drugs
|
...
|
|
Most frequent route of metabolism
|
Hepatic enzymes
|
|
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
|
Sodium channel blockade
|
|
MOA for benzodiazepines and barbiturates
|
GABA-related targets
|
|
MOA for Ethosuximide
|
Calcium channels
|
|
MOA for Valproic acid at high doses
|
Affect calcium, potassium, and sodium channels
|
|
Drugs of choice for generalized tonic-clonic and partial seizures
|
Valproic acid and Phenytoin
|
|
DOC for febrile seizures
|
Phenobarbital
|
|
Drugs of choice for absence seizures
|
Ethosuximide and valproic acid
|
|
Drug of choice for myoclonic seizures
|
Valproic acid
|
|
Drugs of choice for status epilepticus
|
IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy
|
|
Drugs that can be used for infantile spasms
|
Corticosteroids
|
|
Anti-seizure drugs used also for bipolar affective disorder (BAD)
|
Valproic acid, carbamazepine, phenytoin and gabapentin
|
|
Anti-seizure drugs used also for Trigeminal neuralgia
|
Carbamazepine
|
|
Anti-seizure drugs used also for pain of neuropathic orgin
|
Gabapentin
|
|
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
|
Phenytoin
|
|
SE of phenytoin
|
Gingival hyperplasia, nystagmus, diplopia and ataxia
|
|
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
|
Carbamazepine
|
|
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
|
Valproic acid
|
|
Laboratory value required to be monitored for patients on valproic acid
|
Serum ammonia and LFT's
|
|
SE for Lamotrigine
|
Stevens-Johnson syndrome
|
|
SE for Felbamate
|
Aplastic anemia and acute hepatic failure
|
|
Anti-seizure medication also used in the prevention of migraines
|
Valproic acid
|
|
Carbamazepine may cause
|
Agranulocytosis
|
|
Anti-seizure drugs used as alternative drugs for mood stabilization
|
Carbamazepine, gabapentin, lamotrigine, and valproic acid
|
|
General Anesthetics
|
...
|
|
MOA of general anesthetics
|
Most are thought to act at GABA-A receptor - chloride channel
|
|
Inhaled anesthetic with a low blood/gas partition coefficient
|
Nitrous oxide
|
|
Inversely related to potency of anesthetics
|
Minimum alveolar anesthetic concentration (MAC)
|
|
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
|
Halothane and methoxyflurane
|
|
Most inhaled anesthetics SE
|
Decrease arterial blood pressure
|
|
Inhaled anesthetics are myocardial depressants
|
Enflurane and halothane
|
|
Inhaled anesthetic causes peripheral vasodilation
|
Isoflurane
|
|
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
|
Halothane
|
|
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
|
Nitrous oxide
|
|
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
|
Methoxyflurane
|
|
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
|
Nitrous oxide
|
|
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
|
Desflurane
|
|
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
|
Dantrolene
|
|
IV barbiturate used as a pre-op anesthetic
|
Thiopental
|
|
Benzodiazepine used adjunctively in anesthesia
|
Midazolam
|
|
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
|
Flumazenil
|
|
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
|
Ketamine
|
|
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
|
Fentanyl
|
|
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
|
Neuroleptanesthesia
|
|
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
|
Propofol
|
|
Local Anesthetics
|
...
|
|
MOA of local anesthetics (LA's)
|
Block voltage-dependent sodium channels
|
|
This may enhance activity of local anesthetics
|
Hyperkalemia
|
|
This may antagonize activity of local anesthetics
|
Hypercalcemia
|
|
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
|
Vasodilation
|
|
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
|
Cocaine
|
|
Longer acting local anesthetics which are less dependent on vasoconstrictors
|
Tetracaine and bupivacaine
|
|
These LA's have surface activity
|
Cocaine and benzocaine
|
|
Most important toxic effects of most local anesthetics
|
CNS toxicity
|
|
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
|
Cocaine
|
|
LA causing methemoglobinemia
|
Prilocaine
|
|
Skeletal Muscle Relaxants
|
...
|
|
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
|
Neuromuscular blocking drugs
|
|
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
|
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
|
|
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
|
Nondepolarizing type antagonists
|
|
Agent with long duration of action and is most likely to cause histamine release
|
Tubocurarine
|
|
Non-depolarizing skeletal muscle antagonist that has short duration
|
Mivacurium
|
|
Skeletal muscle agent that can block muscarinic receptors
|
Pancuronium
|
|
Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
|
Atracurium
|
|
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
|
Succinylcholine
|
|
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
|
Cholinesterase inhibitors
|
|
Spasmolytic drugs
|
...
|
|
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
|
Spasmolytic drugs
|
|
Facilitates GABA presynaptic inhibition
|
Diazepam
|
|
GABA agonist in the spinal cord
|
Baclofen
|
|
Similar to clonidine and may cause hypotension
|
Tizanidine
|
|
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
|
Dantrolene
|
|
Agent used for acute muscle spasm
|
Cyclobenzaprine
|
|
Drugs Used in Parkinsonism & Other Movement Disorders
|
...
|
|
Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
|
Drug induced Parkinsonism
|
|
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
|
L-dopa
|
|
This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
|
Carbidopa
|
|
Clinical response that may fluctuate in tx of Parkinson's dx
|
"On-off-phenomenon"
|
|
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
|
Levodopa
|
|
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
|
Bromocriptine
|
|
Non ergot agents used as first-line therapy in the initial management of Parkinson's
|
Pramipexole and ropinirole
|
|
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
|
Amantadine
|
|
Inhibitor of MAO type B which slows down metabolism of dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
|
Selegiline
|
|
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
|
Tolcapone
|
|
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
|
Benztropine
|
|
Agent effective in physiologic and essential tremor
|
Propranolol
|
|
Agents used in Huntington's Disease
|
Tetrabenazine (amine depleting drug), reserpine
|
|
Agents used in Tourette's dx
|
Haloperidol, pimozide , clonidine
|
|
Chelating agent used in Wilson's disease
|
Penicillamine
|
|
...
|
...
|
|
Antipsychotics
|
...
|
|
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
|
Older antipsychotic agents, D2 receptors
|
|
MOA of neuroleptics
|
Dopamine blockade
|
|
Side effects occuring in antipsychotics that block dopamine
|
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
|
|
Antipsychotics that reduce positive symptoms only
|
Older antipsychotics
|
|
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
|
Olanzapine, aripiprazole, and sertindole
|
|
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
|
Risperidone
|
|
Atypical antipsychotic causing high prolactin levels
|
Risperidone
|
|
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
|
Olanzapine
|
|
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
|
Haloperidol
|
|
Drug used in neuroleptic malignant syndrome
|
Dantrolene
|
|
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
|
Muscarinic blockers
|
|
Antipsychotic having the strongest autonomic effects
|
Thioridazine
|
|
Antipsychotic having the weakest autonomic effects
|
Haloperidol
|
|
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
|
Thioridazine
|
|
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
|
Clozapine
|
|
Anti-psychotic not shown to cause tardive dyskinesia
|
Clozapine
|
|
Anti-psychotics available in depot preparation
|
Fluphenazine and haloperidol
|
|
Reduced seizure threshold
|
Low-potency typical antipsychotics and clozapine
|
|
Orthostatic hypotension and QT prolongation
|
Low potency phenothiazines and ziprasidone
|
|
Increased risk of developing cataracts
|
Quetiapine
|
|
Lithium
|
...
|
|
Major route of elimination for Lithium
|
Kidneys
|
|
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
|
Lithium toxicity
|
|
Drug increases the renal clearance hence decreases levels of lithium
|
Theophylline
|
|
Lithium is associated with this congenital defect
|
Cardiac anomalies and is contraindicated in pregnancy or lactation
|
|
DOC for bipolar affective disorder
|
Lithium
|
|
Concern using lithium
|
Low therapeutic index
|
|
SE of lithium
|
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
|
|
Antidepressants
|
...
|
|
Example of three antidepressants that are indicated for obsessive compulsive disorder
|
Clomipramine, fluoxetine and fluvoxamine
|
|
Neurotransmitters affected by the action of antidepressants
|
Norepinephrine and serotonin
|
|
Usual time needed for full effect of antidepressant therapy
|
2 to 6 weeks
|
|
Population group especially sensitive to side effects of antidepressants
|
Elderly patients
|
|
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
|
Side-effect profile, drug interaction potential and prior pt response
|
|
Well-tolerated and are first-line antidepressants
|
SSRI's, bupropion, and venlafaxine
|
|
Monoamine oxidase inhibitors (MAOI)
|
...
|
|
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
|
Monamine oxidase inhibitors
|
|
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
|
Hypertensive crisis
|
|
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
|
Serotonin syndrome
|
|
Tricyclic antidepressants (TCA)
|
...
|
|
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
|
Tricyclic antidepressants (TCA)
|
|
Three C's associated with TCA toxicity
|
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
|
|
Agents having higher sedation and antimuscarinic effects than other TCA's
|
Tertiary amines
|
|
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
|
Amitriptyline
|
|
TCA used in chronic pain, enuresis, and ADD
|
Imipramine
|
|
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
|
Doxepin
|
|
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
|
Clomipramine
|
|
Secondary amines that have less sedation and more excitation effect
|
Nortriptyline, Desipramine
|
|
Side effects seen with tricyclic antidepressants
|
Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
|
|
Heterocyclics
|
...
|
|
Antidepressant associated with neuroleptic malignant syndrome
|
Amoxapine
|
|
Antidepressant associated with seizures and cardiotoxicity
|
Maprotiline
|
|
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
|
Venlafaxine
|
|
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
|
Venlafaxine, duloxetine
|
|
Antidepressant also used for sleep that causes priapism
|
Trazodone
|
|
Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
|
Nefazodone
|
|
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
|
Bupropion
|
|
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
|
Mirtazapine
|
|
SE of mirtazapine
|
Liver toxicity, increased serum cholesterol
|
|
Selective serotonin reuptake inhibitors (SSRI)
|
...
|
|
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
|
Citalopram and its metabolite escitalopram
|
|
Side effects frequently seen with SSRIs
|
CNS stimulation; GI upset
|
|
Antidepressants with no effect on BP, no sedation
|
SSRIs
|
|
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
|
Fluoxetine
|
|
SSRI indicated for premenstrual dysphoric disorder
|
Fluoxetine (Sarafem)
|
|
Some of SSRIs' therapeutic effects beside depression
|
Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD
|
|
SSRI less likely to cause a withdrawal syndrome
|
Fluoxetine
|
|
Opioid Analgesics & Antagonists
|
...
|
|
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
|
Ascending pathways
|
|
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
|
Presynaptic mu, delta, and kappa receptors
|
|
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
|
Postsynaptic Mu receptors
|
|
Tolerance to all effects of opioid agonists can develop except
|
Miosis and constipation
|
|
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
|
Meperidine
|
|
SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
|
Opioid Analgesics
|
|
Strong opioid agonists
|
Morphine, methadone, meperidine, and fentanyl
|
|
Opioids used in anesthesia
|
Morphine and fentanyl
|
|
Opioid used in the management of withdrawal states
|
Methadone
|
|
Opioid available trans-dermally
|
Fentanyl
|
|
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
|
Morphine
|
|
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
|
Meperidine
|
|
Moderate opioid agonists
|
Codeine, hydrocodone, and oxycodone
|
|
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
|
Propoxyphene
|
|
Partial agonist or mixed antagonists
|
...
|
|
Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
|
Buprenorphine
|
|
Opioid antagonist that is given IV and had short DOA
|
Naloxone
|
|
Opioid antagonist that is given orally in alcohol dependency programs
|
Naltrexone
|
|
These agents are used as antitussive
|
Dextromethorphan, Codeine
|
|
These agents are used as antidiarrheal
|
Diphenoxylate, Loperamide
|
|
Drugs of Abuse
|
...
|
|
Inhalant anesthetics
|
NO, chloroform, and diethyl ether
|
|
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
|
Fluorocarbons and Industrial solvents
|
|
Cause dizziness, tachycardia, hypotension, and flushing
|
Organic nitrites
|
|
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
|
Steroids
|
|
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
|
Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
|
|
Opioid Analgesics
|
...
|
|
Most commonly abused in health care professionals
|
Heroin, morphine, oxycodone, meperidine and fentanyl
|
|
This route is associated with rapid tolerance and psychologic dependence
|
IV administration
|
|
Leads to respiratory depression progressing to coma and death
|
Overdose of opioids
|
|
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
|
Abstinence syndrome
|
|
Treatment for opioid addiction
|
Methadone, followed by slow dose reduction
|
|
This agent may cause more severe, rapid and intense symptoms to a recovering addict
|
Naloxone
|
|
Sedative-Hypnotics
|
...
|
|
Sedative-Hypnotics action
|
Reduce inhibition, suppress anxiety, and produce relaxation
|
|
Additive effects when Sedative-Hypnotics used in combination with these agents
|
CNS depressants
|
|
Common mechanism by which overdose result in death
|
Depression of medullary and cardiovascular centers
|
|
"Date rape drug"
|
Flunitrazepam (rohypnol)
|
|
The most important sign of withdrawal syndrome
|
Excessive CNS stimulation (seizures)
|
|
Treatment of withdrawal syndrome involves
|
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
|
|
These agents are CNS depressants
|
Ethanol, Barbiturates, and Benzodiazepines
|
|
Stimulants
|
...
|
|
Withdrawal from this drug causes lethargy, irritability, and headache
|
Caffeine
|
|
W/D from this drug causes anxiety and mental discomfort
|
Nicotine
|
|
Treatments available for nicotine addiction
|
Patches, gum, nasal spray, psychotherapy, and bupropion
|
|
Chronic high dose abuse of nicotine leads to
|
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
|
|
Tolerance is marked and abstinence syndrome occurs
|
Amphetamines
|
|
Amphetamine agents
|
Dextroamphetamines and methamphetamine
|
|
These agents are congeners of Amphetamine
|
DOM, STP, MDA, and MDMA "ecstasy"
|
|
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
|
Cocaine "super-speed"
|
|
Hallucinogens
|
...
|
|
Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic
|
PCP
|
|
Removal of PCP may be aided
|
Urinary acidification and activated charcoal or continual nasogastric suction
|
|
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
|
Marijuana
|
|
Cholinoreceptor-Activating & Cholinesterase-Inhibiting Drugs
|
...
|
|
Direct-Acting Cholinomimetic Agonists
|
...
|
|
Muscarinic agonists or parasympathomimetic
|
...
|
|
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
|
Bethanechol
|
|
Only direct acting agent that is very lipid soluble and used in glaucoma
|
Pilocarpine
|
|
This agent used to treat dry mouth in Sjögren's syndrome
|
Cevimeline
|
|
Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
|
Edrophonium
|
|
Carbamate with intermediate action, used for postoperative and neurogenic ileus and urinary retention
|
Neostigmine
|
|
Treatment of atropine overdose and glaucoma (because lipid soluble). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
|
Physostigmine
|
|
Long-term treatment of myasthenia gravis
|
Pyridostigmine
|
|
Organophosphates
|
...
|
|
Antiglaucoma organophosphate
|
Echothiophate
|
|
Associated with an increased incidence of cataracts in patients treated for glaucoma
|
Long acting cholinesterase inhibitors
|
|
Scabicide organophosphate
|
Malathion
|
|
Organophosphate anthelmintic agent with long DOA
|
Metrifonate
|
|
Toxicity of organophosphate:
|
DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
|
|
The most frequent cause of acute deaths in cholinesterase inhibitor toxicity
|
Respiratory failure
|
|
The most toxic organophosphate
|
Parathion
|
|
Treatment of choice for organophosphate overdose
|
Atropine
|
|
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
|
Pralidoxime
|
|
Cholinoreceptor Blockers & Cholinesterase Regenerators
|
...
|
|
Prototypical drug is atropine
|
Nonselective Muscarinic Antagonists
|
|
Treat manifestations of Parkinson's disease and EPS
|
Benztropine, trihexyphenidyl
|
|
Treatment of motion sickness
|
Scopolamine, meclizine
|
|
Produce mydriasis and cycloplegia
|
Atropine, homatropine,C1208 tropicamide
|
|
Bronchodilation in asthma and COPD
|
Ipratropium
|
|
Reduce transient hyper GI motility
|
Dicyclomine, methscopolamine
|
|
Cystitis, postoperative bladder spasms, or incontinence
|
Oxybutynin, dicyclomine
|
|
Toxicity of anticholinergics
|
block SLUD (salivation, lacrimation, urination, defecation)
|
|
Another mnemonic for anticholinergic toxicity
|
"dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
|
|
Atropine fever is the most dangerous effect and can be lethal in this population group
|
Infants
|
|
Contraindications to use of atropine
|
Infants, closed angle glaucoma, prostatic hypertrophy
|
|
Nicotinic Antagonists
|
...
|
|
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
|
Severe hypertension
|
|
Reversal of blockade by neuromuscular blockers
|
Cholinesterase inhibitors
|
|
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
|
Nondepolarizing Neuromuscular Blockers
|
|
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use; has short duration of action
|
Succinylcholine
|
|
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
|
Cholinesterase regenerators, pralidoxime
|
|
Used to treat patients exposed to insecticides such as parathion
|
Pralidoxime, atropine
|
|
Sympathomimetics
|
...
|
|
Mnemonic for beta receptors
|
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
|
|
This is the drug of choice for anaphylactic shock
|
Epinephrine
|
|
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
|
Amphetamines
|
|
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
|
Phenylephrine
|
|
Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma by acting to
|
Reduce aqueous secretion
|
|
Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis
|
Albuterol
|
|
Longer acting Beta 2 agonist is recommended for prophylaxis of asthma
|
Salmeterol, formoterol (both in combination with corticosteroid; contraindicated as monotherapy)
|
|
These agents increase cardiac output and may be beneficial in treatment of acute heart failure and some types of shock
|
Beta1 agonists
|
|
These agents decrease blood flow or increase blood pressure, are local decongestants, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
|
Alpha1 agonists
|
|
Shock due to septicemia or myocardial infarction is made worse by
|
Increasing afterload and tissue perfusion declines
|
|
Epinephrine is often mixed with a local anesthetic to
|
Reduce the loss from area of injection
|
|
Chronic orthostatic hypotension can be treated with
|
Midodrine
|
|
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
|
Terbutaline
|
|
Sympathetic agent which stimulates heart rate and can dilate vessels in skeletal muscle at low doses
|
Epinephrine
|
|
Mast cells to reduce release of hisamine and inflammatory mediators
|
Epinephrine
|
|
Agent used in shock because it dilates coronary arteries and increases renal blood flow
|
Dopamine
|
|
Agent which stimulates cardiac contractile force more than rate with little effect on total peripheral resistance
|
Dobutamine
|
|
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
|
Ephedrine
|
|
Alpha 1 agonist toxicity
|
Hypertension
|
|
Beta 1 agonist toxicity
|
Sinus tachycardia and serious arrhythmias
|
|
Beta 2 agonist toxicity
|
Skeletal muscle tremor, tachycardia
|
|
The selective agents loose their selectivity at
|
high doses
|
|
Adrenoceptor Blocker
|
...
|
|
Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis
|
Phenoxybenzamine
|
|
Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena
|
Phentolamine
|
|
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
|
Prazosin, terazosin, doxazosin
|
|
Selective Alpha-1A blocker, used for BPH, but with little effect on HTN
|
Tamsulosin
|
|
Selective Alpha 2 blocker used for impotence (controversial effectiveness)
|
Yohimbine
|
|
Beta-Blocking Drugs
|
...
|
|
SelectiveB1 Receptor blockers that may be useful in treating patients even though they have asthma
|
Acebutolol, atenolol, esmolol, metoprolol
|
|
Combined alpha and beta blocking agents that may have application in treatment of CHF
|
Labetalol and carvedilol
|
|
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma
|
Pindolol and acebutolol
|
|
This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
|
Timolol
|
|
This parenteral beta blocker is a short acting (minutes)
|
Esmolol
|
|
This beta blocker is the longest acting
|
Nadolol
|
|
These beta blockers are less lipid soluble
|
Acebutolol and atenolol
|
|
This beta blocker is highly lipid soluble and may account for side effects such as nightmares
|
Propranolol
|
|
Clinical uses of these agents include treatment of HTN, angina, arrhythmias, chronic CHF, and selected post MI patients
|
Beta blockers
|
|
Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF; signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety)
|
Beta blockers
|
|
Glaucoma (all agents topical except for diuretics)
|
...
|
|
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
|
Pilocarpine, carbachol, physostigmine
|
|
Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins
|
Epinephrine, dipivefrin
|
|
Selective alpha agonists that decreases aqueous secretion
|
Apraclonidine, brimonidine
|
|
These Beta blockers decrease aqueous secretion
|
Timolol (nonselective), betaxolol (selective)
|
|
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis
|
Acetazolamide
|
|
This agent cause increased aqueous outflow
|
Prostaglandin PGF2a
|
|
Antihypertensive Agents
|
...
|
|
Inhibit peptidyl dipeptidase (plasma kininase)
|
ACE inhibitors
|
|
SE of ACE inhibitors
|
Cough, hyperkalemia, angioedema
|
|
ACE inhibitors are contraindicated in
|
pregnancy and with K+
|
|
Losartan and valsartan block
|
Angiotensin AT1 receptor
|
|
Angiotensin receptor blockers do NOT effect
|
Bradykinin metabolism
|
|
Agents that block L-type calcium channel
|
Calcium channel blockers
|
|
CCB contraindicated in CHF
|
Verapamil
|
|
CCB with predominant effect on vasodilation
|
Nifedipine
|
|
SE of CCB
|
atrioventricular block, constipation, edema
|
|
Agents that reduce heart rate, contractility, and O2 demand
|
Beta-blockers
|
|
B-blockers that are more cardioselective
|
Beta-1 selective blockers (AMEBBA - atenolol, metoprolol, esmolol, betaxolol, bisoprolol, acebutalol)
|
|
Beta-blockers should be used cautiously in
|
Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
|
|
Non-selective Beta-blocker also used for migraine prophylaxis
|
Propranolol
|
|
SE of beta blockers
|
Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
|
|
Alpha 1selective blockers
|
Prazosin, terazosin and doxazosin (-AZOSIN ending)
|
|
Non-selective Alpha1blockers use to treat pheochromocytoma
|
Phenoxybenzamine
|
|
For rebound HTN from rapid clonidine withdrawal
|
Phentolamine
|
|
SE of alpha blockers
|
Orthostatic hypotension (especially with first dose) and reflex tachycardia
|
|
Partial Alpha agonist used in HTN, acts centrally
|
Clonidine
|
|
Used primarily for hypertension during pregnancy, can give positive Coomb's test
|
Methyldopa
|
|
SE of clonidine
|
sedation, dry mouth, mental depression
|
|
Direct vasodilator of arteriolar smooth muscle
|
Hydralazine
|
|
SE of hydralazine with slow acetylators
|
Lupus-like syndrome
|
|
Arterial vasodilator that works by opening K+ channels
|
Minoxidil
|
|
SE of minoxidil
|
Hypertrichosis
|
|
IV Drug used Hypertensive Crisis
|
Nitroprusside, fenoldopam, labetalol
|
|
Nitroprusside vasodilates
|
Arteries and veins
|
|
Toxicity caused by nitroprusside and treatment
|
Cyanide toxicity treated with sodium thiosulfate
|
|
Diuretics
|
...
|
|
Carbonic anhydrase inhibitor
|
Acetazolamide
|
|
Diuretic used for mountain sickness and glaucoma
|
Acetazolamide
|
|
SE of acetazolamide
|
Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
|
|
MOA of loop diuretics
|
inhibits Na+/K+/2Cl- cotransport
|
|
Site of action of loop diuretics
|
Thick ascending limb
|
|
SE of loop (furosemide) diuretics
|
Hyperuricemia, hypokalemia and ototoxicity
|
|
Aminoglycosides used with loop diuretics potentiate adverse effect
|
Ototoxicity
|
|
Loops lose and thiazide diuretics retain
|
Calcium
|
|
MOA of thiazide diuretics
|
Inhibit Na+/Cl- cotransport
|
|
Site of action of thiazide diuretics
|
Work at early distal convoluted tubule
|
|
Class of drugs that may cause cross-sensitivity with thiazide diuretics
|
Sulfonamides
|
|
SE of thiazide (HCTZ) diuretics
|
Hyperuricemia, hypokalemia and hyperglycemia
|
|
Potassium sparing diuretics inhibit
|
Na+/K+ exchange
|
|
Diuretic used to treat primary aldosteronism
|
Spironolactone
|
|
SE of spironolactone
|
Gynecomastia, hyperkalemia
|
|
Osmotic diuretic used to treat increased intracranial pressure
|
Mannitol
|
|
Antidiuretic hormone (ADH) agonist and antagonist
|
...
|
|
ADH agonist used for pituitary diabetes insipidus
|
Desmopressin (DDAVP)
|
|
Used for SIADH
|
Demeclocycline
|
|
SE of demeclocycline
|
Bone marrow and teeth discoloration for children under 8 years of age
|
|
Antiarrhythmic agents
|
...
|
|
MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
|
Sodium channel blockers
|
|
SE of procainamide
|
Lupus-like syndrome
|
|
Limiting side effect of Quinidine
|
Prolongs QT interval
|
|
Other side effects of Quinidine
|
Thrombocytopenic purpura, and CINCHONISM
|
|
Major drug interaction with Quinidine
|
Increases concentration of Digoxin
|
|
DOC for management of acute ventricular arrhythmias
|
Amiodarone
|
|
DOC for digoxin induced arrhythmias
|
Phenytoin
|
|
SE of phenytoin
|
Gingival hyperplasia
|
|
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents
|
Class IC (flecainide, propafenone, moricizine)
|
|
Class II antiarrhythmics are
|
B-blockers
|
|
Antiarrhythmic that exhibits Class II and III properties
|
Sotalol
|
|
Side effect of sotalol
|
prolongs QT and PR interval
|
|
Used intravenously for acute arrhythmias during surgery
|
Esmolol
|
|
Anti-arrhythmics that decrease mortality
|
B-blockers
|
|
MOA of class III antiarrhythmics
|
Potassium channel blockers
|
|
Class III antiarrhythmic that exhibits properties of all 4 classes
|
Amiodarone
|
|
Specific pharmacokinetic characteristic of amiodarone
|
Prolonged half-life, up to six weeks
|
|
Antiarrhythmic effective in most types of arrhythmia
|
Amiodarone
|
|
SE of Amiodarone
|
Cardiac dysfunction, photosensitivity, skin (blue smurf syndrome), Pulmonary fibrosis, thyroid and corneal deposits
|
|
MOA of class IV antiarrhythmics
|
Calcium channel blockers
|
|
Life threatening cardiac event that prolong QT leads to
|
Torsades de pointes
|
|
Agent to treat torsades de pointes
|
Magnesium sulfate
|
|
Drug used supraventricular arrhythmias
|
Digoxin
|
|
DOC for paroxysmal supraventricular tachycardia (PSVT)
|
Adenosine
|
|
Adenosine's MOA
|
Activattion on an inward K+ current and inhibition of Ca++ current resulting in marked hyperpolarization
|
|
Anti-arrhythmic with 15 second duration of action
|
Adenosine
|
|
Vasodilators and treatment of angina
|
...
|
|
MOA of sildenafil (Viagra)
|
Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP
|
|
Drugs used in the management of angina
|
Aspirin, Nitrates, CCB, and Beta blockers
|
|
Aspirin reduces mortality in unstable angina by
|
Platelet aggregation inhibition
|
|
MOA of nitrates
|
Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles
|
|
Nitrate used for acute anginal attacks
|
Nitroglycerin sublingual tablets
|
|
Nitrate used to prevent further attacks
|
Oral and transdermal forms of nitroglycerin
|
|
Nitrate free intervals are needed due to
|
Tolerance
|
|
SE of nitrates
|
Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation
|
|
CCB are DOC for
|
Prinzmetal's angina
|
|
Beta blockers are used for which type of anginal attack
|
Classic
|
|
Drugs used to treat CHF
|
...
|
|
MOA of Cardiac glycosides (eg. digoxin)
|
Indirectly increase intracellular calcium and cardiac contractility by inhibiting Na+/K+ ATPase
|
|
...
|
...
|
|
Digoxin is used in
|
Atrial fibrillation and CHF
|
|
Digoxin toxicity can be precipitated by
|
Hypokalemia
|
|
Antidote for digoxin toxicity
|
Digoxin immune fab
|
|
Drug used for moderate to severe heart failure, reduces mortality, especially for patients taking digitalis to prevent hypokalemia
|
Spironolactone, Eplerenone
|
|
Combination recommended for only African Americans to reduce preload and afterload in CHF
|
Isosorbide dinitrate/hydralazine
|
|
Beta 1 agonists used iv in acute decompensated HF
|
Dobutamine and dopamine
|
|
Diuretics work in CHF by
|
Reducing preload
|
|
Beta blockers work in CHF by
|
Reducing adverse effects of high catecholamine levels on heart (never use in acute heart failure)
|
|
Dual ARB and neprilysin inhibitor, early phase 2 trial for heart failure and hypertension
|
LCZ696, sucabitril
|
|
Select group of beta blockers that reduce heart failure mortality
|
Carvedilol, metoprolol, bisoprolol, nebivolol
|
|
Vasodilator used in acute CHF resembling brain natriuretic peptide
|
Nesiritide (Natrecor)
|
|
Drugs used in coagulation disorders
|
...
|
|
Vitamin K dependent anticoagulant
|
Warfarin (PT)
|
|
Warfarin is contraindicated in
|
Pregnancy
|
|
Anticoagulant of choice in pregnancy
|
Heparin
|
|
Heparin (PTT) increases activity of
|
Antithrombin 3
|
|
Route of administration of warfarin
|
Oral
|
|
Routes of administration of heparin
|
IV and IM (only LMW)
|
|
SE of both warfarin and heparin
|
Bleeding
|
|
SE of heparin
|
Heparin induced thrombocytopenia (HIT)
|
|
Alternative anticoagulant used if HIT develops
|
Lepirudin
|
|
Antidote to reverse actions of warfarin
|
Vitamin K or fresh frozen plasma
|
|
Antidote to reverse actions of heparin
|
Protamine sulfate
|
|
MOA of aspirin
|
Irreversibly blocking cyclooxygenase
|
|
Agent used to treat MI and to reduce incidence of subsequent MI
|
Aspirin, metoprolol
|
|
SE of Aspirin
|
GI bleeding
|
|
Antiplatelet drug reserved for patients allergic to aspirin
|
Ticlopidine
|
|
SE for ticlopidine
|
Neutropenia and agranulocytosis
|
|
Effective in preventing TIA's
|
Clopidogrel and ticlopidine
|
|
Prevents thrombosis in patients with artificial heart valve
|
Dipyridamole
|
|
Block glycoprotein IIb/IIIa involved in platelet cross-linking
|
Abciximab, tirofiban and eptifibatide
|
|
MOA of thrombolytics
|
Degradation of fibrin clots and are administered IV
|
|
Thrombolytics are used for
|
Pulmonary embolism and DVT
|
|
Thrombolytic that can cause allergic reaction
|
Streptokinase
|
|
Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA
|
Tissue plasmin activator
|
|
SE of tPA
|
Cerebral hemorrhage
|
|
Antidote for thrombolytics
|
Aminocaproic acid
|
|
Agents used in anemias and hematopoietic growth factors
|
...
|
|
Agent to treat hypochromic microcytic anemias
|
Ferrous sulfate
|
|
Chelating agent used in acute iron toxicity
|
Deferoxamine
|
|
Agent for pernicious anemia
|
Cyanocobalamin (Vit B12)
|
|
Agent used for neurological deficits in megaloblastic anemia
|
Vitamin B12
|
|
Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy
|
Folic acid
|
|
Agent used for anemias associated with renal failure
|
Erythropoietin agonists
|
|
Agent used neutropenia especially after chemotherapy
|
G-CSF (filgrastim) and GM-CSF (sargramostim)
|
|
Treatment of patients with prior episodes of thrombocytopenia after a cycle of cancer chemotherapy
|
Interleukin 11 (oprelvekin)
|
|
Antihyperlipidemics
|
...
|
|
Drugs decrease intestinal absorption of cholesterol
|
Bile acid-binding resins
|
|
Cholestyramine and colestipol are
|
Bile acid-binding resins
|
|
Major nutritional side effect of bile acid-binding resins
|
Impair absorption of fat soluble vitamin absorption (A,D,E,K)
|
|
MOA of lovastatin (STATIN)
|
inhibits HMG COA reductase
|
|
HMG CoA reductase inhibitors are contraindicated in
|
Pregnancy
|
|
MOA of drug or foods (grapefruit juice) that increase statin effect
|
Inhibit Cytochrome P450 3A4
|
|
SE of HMG COA reductase inhibitors
|
Rhabdomyolysis and Hepatotoxicity
|
|
Monitoring parameter to obtain before initiation of STATINS
|
LFT's
|
|
Decreases liver triglycerol synthesis
|
Niacin
|
|
SE of niacin
|
Cutaneous flush
|
|
Cutaneous flush can be reduced by pretreatment with
|
Aspirin
|
|
Fibrates (gemfibrozil) increase activity of
|
Lipoprotein lipase
|
|
Most common SE of fibrates
|
Nausea
|
|
Fibrates are contraindicated in
|
Pregnancy
|
|
Concurrent use of fibrates (gemfibrozil) and statins (simvastatin, lovastatin) increases risk of
|
Rhabdomyolysis
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
|
Ezetimibe (Zetia)
|
|
NSAIDS and DMARDS
|
...
|
|
MOA of NSAIDS
|
inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)
|
|
Difference between aspirin and other NSAIDS
|
Aspirin irreversibly inhibits cyclooxygenase
|
|
Four main actions of NSAIDS
|
Anti-inflammatory, analgesia, antipyretic and antiplatelet activity
|
|
Agent used for closure of patent ductus arteriosus
|
Indomethacin
|
|
Aspirin is contraindicated in children with viral infection
|
Potential for development of Reye's syndrome
|
|
SE of salicylates
|
Tinnitus, GI bleeding
|
|
NSAID also available as an ophthalmic preparation
|
Diclofenac, ketoralac
|
|
NSAID available orally, IM and ophthalmically
|
Ketorolac
|
|
NSAID that is used for acute condition, such as post-surgical pain and has limited duration (<5 days) of use due to nephrotoxicity
|
Ketorolac
|
|
Newer NSAID that selectively inhibits COX-2
|
Celecoxib
|
|
COX 2 inhibitors may have reduced risk of
|
Gastric ulcers and GI Bleeding
|
|
COX 2 inhibitors should be used cautiously in pts with
|
Pre-existing cardiac or renal disease
|
|
Acetaminophen only has
|
Antipyretic and analgesic activity
|
|
SE of acetaminophen
|
Hepatotoxicity
|
|
Antidote for acetaminophen toxicity
|
N-acetylcysteine
|
|
Drugs-Modifying Anti-Rheumatic Agents (DMARDS)
|
...
|
|
DMARDs are slow acting drugs for
|
Rheumatic disease
|
|
Initial DMARD of choice for patients with RA
|
Methotrexate
|
|
Drug ofter used in combination with TNF - alpha inhitors for RA
|
Methotrexate
|
|
Causes bone marrow suppression
|
Azathioprine
|
|
Interferes with activity of T-lymphocytes
|
Hydroxychloroquine
|
|
Anti-malarial drug used in rheumatoid arthritis (RA)
|
Hydroxychloroquine
|
|
SE of hydroxychloroquine
|
Retinal destruction and dermatitis
|
|
MOA of Leflunomide (newer agent)
|
Inhibiting dihydroorotate dehydrogenase which leads to decreased pyrimidine synthesis, decreased T cell proliferation and decreased antibody production by B cells
|
|
Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha)
|
Adalimumab, infliximab and etanercept
|
|
Anti-rheumatic agent also used for ulcerative colitis
|
Sulfasalazine
|
|
Anti-rheumatic agent also used for Chron's disease
|
Infliximab
|
|
Drugs used in Gout
|
...
|
|
NSAID used in gout
|
Indomethacin
|
|
NSAID contraindicated in gout
|
Aspirin
|
|
MOA of colchicine (used in acute gout)
|
Selective inhibitor of microtubule assembly
|
|
SE of colchicine
|
Kidney and liver toxicity, diarrhea
|
|
Agent used to treat chronic gout by increasing uric acid secretion and excretion
|
Probenecid and sulfinpyrazone
|
|
Allopurinol treats chronic gout by decreasing uric acid production by inhibiting
|
Xanthine oxidase
|
|
Insulins
|
...
|
|
Rapid acting insulins that do not self-aggregate
|
lispro insulin, aspart insulin, glulisine insulin
|
|
Peakless long acting insulin
|
Insulin glargine
|
|
Cardiac drugs
|
...
|
|
DOC for paroxysmal supraventricular tachycardia; has high efficacy and short duration of action
|
Adenosine
|
|
Miscellaneous Antimicrobial Agents: Disinfectants, Antiseptics, Sterilants
|
...
|
|
Decontamination of health care worker after caring for patient with C. difficile infection
|
Proper hand-washing with soap and water
|
|
Used to sterilize endoscopes and dental equipment
|
Formaldehyde, glutaraldehyde, ortho-phthalaldehyde, sterilox, hydrogen peroxide, peracetic acid
|
|
Disinfection of blood spills
|
1:10 dilution of household bleach
|
|
Bactericidal, fungicidal, sporicidal disinfectant used to wipe hospital beds
|
1:10 dilution of bleach, phenol
|