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205 Cards in this Set
- Front
- Back
What do you develop w/ benzodiazepines use? What receptors? |
Tolerance
down-regulation of B2 receptors |
|
Initial Tx for Status Epilepticus?
|
1) Diazepam
2) Lorazepam |
|
What drug causes sedation, ataxia and diplopia?
|
Phenytoin
SAD Sx. |
|
What is SAD Sx and who produces it?
|
sedation, ataxia and diplopia
Phenytoin |
|
What drugs causes gingival hyperplasia?
|
1) Phenytoin
2) Nifedipine 3) Cyclosporin |
|
CNS drugs
|
CNS drugs...
|
|
Name the anticonvulsant that is degraded in zero-order?
|
Phenytoin
|
|
What drug is used for tx of abscence seizure?
|
Ethosuximide
|
|
What is the mechanism of action of ethosuximide?
|
blocks Ca+ in thalamic neurons
|
|
What drug do you use for preop sedation i.v.? It causes amnesia...
|
Midazolam
|
|
Name the drug that causes megaloblastic anemia and decreases folic acid?
|
Phenytoin
|
|
What anticovulsant causes SIADH?
|
Carbamazepine
|
|
What effect does carbamazepine have on the liver?
|
it induces cyt P450 (+)
|
|
What is the formula for minimal alveolar anesthetic concentration?
|
MAC= 1/(potency[lipid solubility])
Lipid = potency = 1/MAC |
|
What anticonvulsant causes drug induced Ricketts or ostemalacia?
|
Phenytoin
|
|
DOC for trigeminal neuralgia?
|
Carbamazepine
|
|
What are 3 Side/Effects (S/E)of Carbamazepine?
|
1) Cyt. P450 inducer (+)
2) Hematotoxicity 3) increase ADH (retains water) |
|
What is the effect of carbamazepine and Oral Contraceptives?
|
inactivates sex steroids and O.C.
lowers estriol |
|
What is carbamazepine the DOC for?
|
Trigeminal Neuralgia
|
|
What effect does carbamazepine have on P450?
|
induces it
|
|
Name two important Side/Effects (S/E) of Carbamazepine?
|
1) hematotoxicity
2) SIADH |
|
Drug used for Anxiety/Panic?
|
A/P AlPrazolam
|
|
Patien w/ depression needs to be treated but has liver failure? Tx pt. w/ which benzos...
|
1) Oxazepam
2) Temazepam 3) Lorazepam Out The Liver |
|
What are the three OUT THE LIVER Benzodiazepines?
|
Oxazepam
Temazepam Lorazepam |
|
Tx for Status Epilepticus (I.V.)?
|
Lorazepam
|
|
What drug is used for relaxation and detoxification for withdrawal states?
|
diazepam
|
|
Antidote for Zolpidem overdose?
|
Flumazenil |
|
Where do benzodiazepines work?
|
GABAa receptor
gama binding site BZ1 hypnotic (sleep) increases frecuency of Cl- channel |
|
What site do benzodiazepines act in?
|
gama binding site
BZ 1 |
|
What drug is antagonist at the BZ receptor?
|
flumazenil
|
|
What drug acts in the BZ1 receptor but it's not a benzodiazepine?
|
Zolpidem
|
|
What is the action of barbiturates [high dose]?
|
increase duration Cl-
opens Cl- channels blocks Na+ channels barbiDURATES increases duration of Cl- open |
|
What is the mechanism of Buspirone?
|
- no gaba
- partial agonist at 5HT1a -nonsedating |
|
What is the action of disulfiram? Whic cell compartment does it work on?
Increase what? |
inhibits acetaldehyde dehydrogenase
- mitochondria - increases NADH |
|
What is Methanol used for? (Tx)
|
- Ehtanol intoxication
- fomepizole |
|
What is the definite Tx for ethanol/fomepizole intoxication?
|
Dialysis
|
|
What is methanol degraded to?
Enzyme? |
formaldehyde
- alcohol dehydrogenase |
|
What is the lethal dose of methanol?
|
5 ounces
|
|
What is the toxic retinal dose of methanol?
|
5cc
|
|
What does the Disulfiram Reaction consists of?
|
1) Nausea
2) Vomiting 3) Vertigo 4) Hypotension/Shock |
|
What causes a 3/sec spike pattern on EEG?
|
Abscence seizure
Petite Mal |
|
What is indicated in neuropathic pain?
|
1) Felbamate
2) Lamotrigine 3) Gabapentin |
|
What are the S/E of Felbamate?
|
Aplastic Anemia
Acute Liver Failure |
|
What are the S/E of Lamotrigine?
|
Steven-Jonhson Sx
Rash |
|
What are felbamate, lamotrigine and gabapentin used for?
|
Neuropathic pain
|
|
Name the 3 new Anticovulsants?
|
Felbamate
Lamotrigine Gabapentin |
|
Name 3 drugs used in complex seizure tx?
|
Valproic Acid
Phenytoin Carbamazepine |
|
Tx for Generalized Anxiety States (GAS)?
|
Buspirone
|
|
How long do you wait for buspirone to take effect?
|
1-2 weeks
|
|
What is divalproex used for?
|
Bipolar Disorder (backup)
|
|
What is the mech. of action (M/A) for Divalproex?
|
Ca+ block
inhibits GABA transaminase axonal Na+ block |
|
What are the A/E of Valproic Acid?
|
1) hePAtotoxicity
2) PAncreatitis 3) aloPEcia 4) sPIna Bifida (Teratogenic) PA PE PI VALPA PE PI |
|
What combination w/ anticonvulsants have additive CNS depression?
|
1) antihistamines
2) ethanol 3) sedative-hypnotics 4) opioids |
|
What happens if you withdrawal anticonvulsants abruptly?
|
Seizure might be precipitated
|
|
What is the Tx for Tonic-clonic seizure?
|
- Valproic Acid
- Phenytoin - Carbamazepine |
|
This is unique to collagen?
|
hydroxyproline
|
|
What is the defect in Ehlers-Danlos? name the gene
|
mutation of collagen gene
- lysine hydroxylase gene |
|
What are the symptoms of Ehlers-Danlos
|
hyperextensible, hypermobile joints, dislocations
|
|
What is the defect in Menkes Dz?
|
inhibition of lysyl oxidase
Copper (Cu+) deficiency |
|
What are the symptoms in Menkes Dz?
|
depigmented steely hair
decrease urinary Cu+ |
|
What disease has mutation in collagen I?
|
Osteogenesis Imperfecta
|
|
What are the symptoms for Osteogenesis Imperfecta?
|
Pathologic Fractures
blue sclera collagen problems |
|
Patient with coarse facial features, gingival hyperplasia and macroglosia? Dx?
|
I-Cell Dz
|
|
What enzyme is deficient in I-Cell Dz?
|
phosphotransferase
|
|
Where in the cell is the problem in I-Cell Dz?
|
Golgi apparatus
Manose-6 Residues |
|
What are the symptoms of I-cell Dz?
|
coarse facial features
gingival hyperplasia macroglosia |
|
Patient with deficiency in Leu, Ile and Val amino acids?
|
Maple Syrup Dz
|
|
What type of amino acids are Leu, Ile and Val?
|
Branched Amino Acids
|
|
What drug inhibits activation? binds to t-RNA with ribosome?
|
blocks initiation
Aminoglycosdies A first letter of the alphabet |
|
What drug has the mechanism of inhibiting peptidyl transferase?
|
Chloramphenicol
|
|
What drug inhibits aminoacyl-tRNA binding to A site?
Elongation |
Tetracycline
t is for tRNA |
|
What drug inhibits the translocation of tRNA?
E.F.3 |
Macr(ol)ides
|
|
What bacteria have the same mechanism of action as macrolides?
|
diphtheria toxin
pseduomonas toxin |
|
What drug is an Angiotensin II blocker?
|
SARTANS
|
|
What are the effects of Sartans on aldosterone, bradykinin, AT-1
|
decrease aldosterone
decrease bradykinin increase AT-1 |
|
What is the DOC (drug of choice) for CHF (Cardiac Heart Failure)?
|
ACE inhibitor
|
|
What effect does ACE have on ATII, bradykinin, aldosterone, fluid, preload, afterload?
|
decrease ATII
increase bradykinin decrease aldosterone decrease fluid increase vasodilation decrease preload decrease afterload |
|
What it the drug used for HTN causes dry cough and angioedema?
|
PRILS [Ace(-)]
|
|
Why do ACE(-) cause cough?
|
increases bradykinin and causes edema in the pharynx
|
|
What drug causes disorientation, visual effects (halos), hallucinations, SVTs, AV block?
|
Digitalis Toxicity
|
|
What enzymes increase cAMP in cardiac cells?
|
(+) adenylyl cyclase
(-) phosphodiesterase III |
|
What is the mechanism of action of sildenafil?
|
blocks PDE V
(-) phosphodiesterase V increases cGMP |
|
What drug interacts with sildenafil?
|
Nitrous Oxide
since NO also increases cGMP |
|
What is the mechanism of phosphodiesterase III? What cells are involved?
|
inhibits conversion of cAMP to AMP
so increase in cAMP Cardiac Cell |
|
What two drugs inhibit PDE III?
|
theophylline
inamirone |
|
What is the mechanism of action of inamirone?
|
blocks cAMP to AMP
incrases cAMP inside cardiac cell increases force of contractilily |
|
What enzymes are deficient in vitamin C def?
|
(-) prolyl and lysyl hydroxylase
|
|
What part of the cell are prolyl and lysyl hydroxylase?
|
inside the R.E.R.
|
|
What is the mechanism of action of dobutamine and dopamine?
|
B1 receptor
increase adenylyl cyclase (+) ATP----> increases cAMP cAMP---> Protein Kinase Protein Kinase opens Ca2+ channels increase in Ca2+ |
|
What is the mechanism of action of digoxin?
|
inhibits Na+/K+ ATPase
decreases sodium/Ca+ exchange Ca+ stays inside the cell to increase contraction force inhibited by K+ increase |
|
What 5 drugs/states cause digitalis toxicity?
|
1) quinidine
2) NSAIDS 3) Amiodarone 4) Verapamil 5) hypokalemia |
|
What is the mechanism of phosphodiesterase V?
|
increases cGMP
blocks breakdown of cGMP--> GMP |
|
What drugs/compounds stimulate Gq to IP3?
|
Acetylcholine (Ach)
Bradykinin 5HT |
|
What happens to Gq after it is converted to IP3?
|
releases Calcium
|
|
What is Calciums effect on Nitrous Oxide?
|
it stimulates the conversion of L-arg to NO
|
|
What amino acid does Nitrous Oxide derive from?
|
L-Arginine
|
|
Where is does the reaction L-Arg to NO take place?
|
endothelium
|
|
What does NO do inside the smooth muscle?
|
stimulates guanylate cyclase
|
|
What does guanulate cyclase stimulate?
|
Conversion of GTP to cGMP
so increase cGMP |
|
What other amino acid is involved in making NO?
|
cysteine
|
|
What does NO stimulate?
|
guanylate cyclase
and conversion of GTP to cGMP increases cGMP |
|
Where in the nephron does acetazolamide act?
|
proximal convoluted tube
|
|
What are the effects of acetazolamide?
|
decreases HCO3-
|
|
What are the toxic effects of acetazolamide?
|
metabollic acidosis
neuropathy, sulfa allergy |
|
What happens to the urine with acetazolamide?
|
increase Na+ excresion
increases HCO3- excresion |
|
What diuretic works in the collecting ducts?
|
Potassium Sparing (K+) diuretics
|
|
What are the K+ sparing diuretics?
|
Spirinolactone
Amiloride Triamterene |
|
How is Spirinolactone different from Amiloride and triamterene?
|
Spirinolactone is an Aldosterone receptor inhibitor
the other two are Na+ Channel blockers |
|
What drug blocks Na+/Cl- symport in the renal system?
|
Thiazides
|
|
What part of the nephron do thiazides act in?
|
Distal Convoluted Tube
DCT |
|
What is used in HTN and Heart Failure (CHF)?
|
Thiazides
|
|
What happens to ions in blood after thiazide administration?
|
Hypokalemia
Alkalosis HyperCAlcemia |
|
What are thiazides used for?
|
HTN and CHF
|
|
What are the toxicities of hydrochorothiazides?
|
hyperGLUC
sulfa allergies |
|
What does hyperGLUC stand for?
|
hyperGlycemia
hyperLipidemia hyperUricemia hyperCalcemia Sulfa Allergies |
|
What is the potential toxicity of K+-Sparing Diuretics?
|
Hyperkalemia
endocrine effects like GYNECOMASTIA! Anti-Androgen |
|
Diuretic that causes hyperglycemia?
|
Thiazide
|
|
What is the mechanism for thiazide acting as hyperglycemia?
|
blocks insulin release
opens K+ Channels keeps insulin inside b-cells |
|
What diurectic causes alkalosis and hypoCalcemia?
|
Loop diuretics
|
|
What diuretic causes alkalosis and hyperCalcemia?
|
Thiazide
|
|
What diuretic causes acidosis and hyperKalemia?
|
K+ sparing
|
|
What diuretic causes acidosis and hypoKalemia?
|
Carbonic Anahydrase inhibitors
|
|
All diuretics cause what?
|
hypokalemia to a degree
except K+ sparing |
|
What is the mechanism of CA(-) Carbonic anahydrase inhibitors?
|
NaHCO3 diuresis
HCO3- decreases in blood so causes H+ to be unbalanced Acidosis |
|
What is the only lipid friendly thiazide?
|
Indapamide
|
|
What diuretics are in the sulfa family?
|
CA(-)
Loops |
|
What diuretic works on ATII? Aldosterone receptor blocker?
|
Spironolactone
|
|
What mechanism does Spirinolactone use? (protein)
|
acts via Zinc Finger Protein
increases gene expression increases Na+ Channels to open |
|
What diuretic causes ginecomastia?
|
Spirinolactone
|
|
Diuretic that causes hypoCAlcemia?
|
Loops
Loops Loose Calcium Tx malignancies with it! |
|
Diuretic that causes hyperCalcemia?
|
Thiazides!
|
|
Question
|
Answer
|
|
Pharmacology Kaplan
|
Pharm
|
|
What drug do Loop diuretics interfere with?
|
Lithium decreases clearance and increases lithium in serum
|
|
What drug potentiates OTOtoxicity w/ Loop diuretics?
|
Aminoglycosides
|
|
What drug interacts w/ Gemfibrozil?
|
HMG-coA reductase inhibitors (statin drugs)
|
|
What is the result of the DDI (drug drug interaction) of Gemfibrozil and Statin drugs?
|
Rhabdomyolisis increases
|
|
What drug potentiates Gemfibrozil?
|
Warfarin and Sulfonylurea
|
|
What drugs inhibit HMG-coA reductase?
|
Statin drugs
|
|
What effect do statin drugs have on cytochrome p450?
|
increases p450 activity p450(+) inducer
|
|
What is the effect of stain drugs on HDL and TGs?
|
HDL increase and decrease in TGs (triclyerides)
|
|
What are the A/E (adverse/effects) of statin drugs?
|
myalgia/myopathy, rhabdomyolysis; p450(+) renal failure; death
|
|
What antilipid drug causes flushing and pruritus (hepatotoxicity)?
|
Nicotinic Acid
|
|
What is the mechanism of action of Cholestipol and Cholestyramine?
|
they are bile acid sequestrants that prevent reabsorption of bile salts in the GI tract
|
|
What is the effect of decrease in bile acid?
|
increase synthesis of new bile salts; decrease liver cholesterol; increase LDL receptors; decrease plasma LDL
|
|
What is contraindicated w/ bile acid sequestrants?
|
concomitant use with hypertriglyceridemias because they increase VLDL and TGs
|
|
What do bile acid sequestrants DDI with?
|
DDI digoxin and warfarin; decrease their absorption
|
|
Does HMG-coA reductase cause SLE Sx?
|
yes
|
|
What ist the mechanism of action of nicotinic acid?
|
inhibits VLDL synthesis and apoprotein synthesis
|
|
What is good about nicotinic acid?
|
increase HDL
|
|
How do you treat the flushing and pruritus w/ nicotinic acid?
|
ASA (aspirin)
|
|
What is another adverse effect of nicotinic acid?
|
hepatotoxicity
|
|
What drug causes flushing, sedation, dyspnea and only acts for t1/2 30 sec?
|
adenosine
|
|
Adenosine is antagonized by?
|
theophilline and caffeine
|
|
Pharmacologist refer to adenosine as?
|
Reset Button Dead for 30 seconds and then heart starts again
|
|
DOC for PSVTs?
|
adenosine
|
|
What are the effects of adenosine on SA and AV?
|
decrease SA and AV; increases AV refractory period
|
|
What drug is an M blocker and is used for asthma and COPD? It has no CNS entry
|
Ipratropium
|
|
It's a cholinomimetic, AchE inhibitor, contracts ciliary m., increases outflow?
|
Pilocarpine and ECHOthiopate
|
|
What are Pilocarpine and Echothiopate used for?
|
Glaucoma
|
|
What are the three K+ channel blockers?
|
Amiodarone, Bretylium and Sotalol ABS system
|
|
What do K+ channel blockers do?
|
slow phase 3, increase APD
|
|
What is the mechanism of action of Quinidine?
|
blocks Na+ channels (decrease I Na); increase APD and ERP; M blocker; alpha block
|
|
DOC for arrythmias following cardioversion? I.V. use
|
Lidocaine
|
|
What is amiodarone used for?
|
Atrial and Ventricular Arrythmias
|
|
What are the S/E of Amiodarone?
|
hepatic necrosis; PULMONARY FIBROSIS; Corneal Deposits; BLUE Pigmentation (SMURF) Skin; Photoxocity; Thyroid Dysfunction
|
|
What is the t1/2 life of Amiodarone?
|
40 days; Largest Vd
|
|
What is Manitol used for?
|
1) maintain renal function; 2) close angle glaucoma; 3) decrease intracraneal pressure (tumor, hematoma)
|
|
Newborn w/ strabysmus, decrease growth, midfacil hypoplasia; microcephaly; CNS Dysfunction; Thin Upperlip (Phyltrum)
|
Fetal Alcohol Syndrome
|
|
What is Benztropine and Trihexyphenidyl used for?
|
Parkinson's; Drug-Induced Extrapyramidal Dysfunction
|
|
Mechanism of action of Benztropine and Trixehyphenidyl?
|
M Blocker
|
|
Drug used in organophosphate poisoning?
|
Pralidoxime
|
|
What does Pralidoxime do w/ symptoms?
|
corrects patients labored breathing and decreases muscle weakness
|
|
What is pralidoxime used for?
|
Organophosphate Poisoning
|
|
What drug is used for Parkinson and Drug-Induced Extrapyramidal Dysfunction?
|
Benztropine and Trihexyphnidyl
|
|
How does alcohol produce gout?
|
Alcohol decreases NADH and increases NAD; increases conversion of reversible reaction pyr ---> Lactate; Lactate increases and competes w/ uric acid excrecion causing gout
|
|
What biochemical compound is increased in alcoholism?
|
NAD+
|
|
What 2 drugs interact with digoxin (DDI)?
|
Quinidine and Verapamil (the queen and the rapper always interfere)
|
|
Drug that causes phototoxicity?
|
Amiodarone
|
|
Name 3 drugs used in AchE inhibitor poisoning?
|
Malathion, Parathion and Sarin (nerve gas)
|
|
What is the MOA of Hydralazine?
|
increase NO
increase Guanylate Cyclase increase cGMP relaxes vascular musculature |
|
What is the effect of Hydralazine on TPR?
|
decreases TPR
involves NO/EDRF pathway decreases resistnace in coronary, renal and cerebral beds |
|
What is hydralazine used for?
|
Tx for moderate to severe HTN
|
|
What is Hydralazine metabolized by?
|
N-acetyltransferase
|
|
What are A/E of hydralazine?
|
headache, flushing, sweating and fluid retention
part of HIP so SLE-like symptoms |
|
What is used in HT emergency?
|
Nitroprusside
|
|
What is the effect of nitroprusside on TPR?
|
decrease TRP via dilation of arterioles and venules
|
|
What happens when there is venule dilation after nitroprusside use?
|
Orthostatic Hypotension
|
|
What are by-products of nitroprusside?
|
thiocyanate and cyanide ions
|
|
What part of the mitochrondria is damaged with cyanide compounds?
|
Comple IV (looks like N)
cyt. a/a3 |
|
What is ethylene glycol?
|
Anti-freeze
|
|
What happens to ethylene glycol once ingested?
|
it is degraded to gycoaldehyde
- Alcohol Dehydrogenase is the enzyme |
|
What comes after degradation of glycoaldehyde?
|
glycolic acid and oxalic acid
latter is nephrotoxic |
|
What causes drug induced SIADH?
|
1) Carbamazepine
2) Chlorpropamide |
|
What are the symptoms in Phenytoin Intoxication?
|
SAD Sx
Sedation Ataxia Diplopia |
|
Name an anticonvulsant that is Zero-Order?
|
Phenytoin
|
|
What condition has an EEG with 3/sec spike pattern?
|
Generalized Abscence Seizure
|
|
What is the Tx for Generalized Abscence Seizure?
|
Ethosuximide
|
|
Name 4 drugs that block voltage gated axonal Na+ influx of fast channels?
|
1) Carbamazepine
2) Phenytoin high dose: 3) Barbiturates 4) Valproic Acid |
|
What drug decreases Ca2+ influx through T channels in thalamic neurons?
|
Ethosuximide
Valproic Acid |
|
What is the action on alpha 2 receptors?
1) NE 2) trasmitter release 3) platelets 4) Pancreas |
1) decrease NE synthesis
2) decrease transmitter release at prejunctional nerve terminals 3) increase aggregation of platelets 4) decrease insulin secretion catabolism |
|
Effect of B1 receptors on renin?
|
increase renin release
|
|
What adrenoreceptor increases insulin secretion?
|
beta 2 receptor stimulation
|
|
What adrenoreceptor induces glycogenolysis?
|
B2 stimulation
|
|
What adrenoreceptor causes uterine relaxation?
|
B2 stimulation
|