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68 Cards in this Set
- Front
- Back
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Major proteins involved in Exocytosis mechanism?
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Synaptobrevin - presynaptic
synaptotagmin - presynaptic Syntaxin - postsynaptic SNAP-25 |
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What are the family types of Botulinum Toxins
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A, B, C1, C2, D, E, F,G
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Which enzymes of the (bot. tox.) proteases family degrade SNAP-25
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A,E
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Which enzymes of the (bot. tox.) proteases family degrade Syntaxin
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C1
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Which enzymes of the (bot. tox.) proteases family degrade Synaptobrevin
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B,D,F,G
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Nicotine will affect simultaneously both sympathetic and parasympathetic systems by...
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BP increase (Sympathetic).
Increase in peristaltic action in the colon (parasympathetic). NA and adrenalin release (Nerves and adrenal gland). |
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Location and mechanism of M1 cholingeric receptors
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Nerves; Gland cells in the stomach
↑IP3, DAG |
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Location and mechanism of M3 cholingeric receptors
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Smooth muscle - contract (Colon, bladder, bronchus)
Secretory glands (saliva, sweat) Endothelial cells - NO synth. & release --> dilation IP3, DAG ↑, via Gq ↑IP3, DAG |
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Location and mechanism of M5 cholingeric receptors
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Nerves in the CNS
(Positive presynaptic feedback) --> ca release ↑IP3, DAG |
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Location and mechanism of M2 cholingeric receptors
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Heart muscle - Open K channels --> K efflux --> hyperpol.
Nerves - GPCR (Gi) , presynaptic neg. feedback - ↓ cAMP |
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Location and mechanism of M4 cholingeric receptors
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Nerves CNS
↓ cAMP (Presynaptic neg. feedback) Open K channels G-protein gated channel |
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Location and mechanism of Nn cholingeric receptors
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ANS gangleons
CNS gangleons Open Na/K channels (ligand gated channel) |
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Location and mechanism of Nm cholingeric receptors
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NMJ
Open Na/K channels ligand gated channel |
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Cholinergic nicotinic receptor (skeletal muscle) - unique subunit?
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ε
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Cholinergic nicotinic receptor (neurons) - unique subunit?
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γ, β
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Cotransmitters accompanying ACh and function?
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ATP - actiavtes purinergic receptors P2y at the edge of the cholinergic nerve and inhibits Ach release.
VIP- vasoactive intestinal peptide Stored in separate vesicles in certain cholinergic neurons and is released with Ach. Acts on smooth muscles and causes their relaxation |
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Action of VIP and ACh in salivary gland
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ATP - saliva secretion
VIP - blood vessel relaxation in gland |
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Cholinergic Muscarinic agonists affect:
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* Internal organs similar to the effects
of the parasympathetic system * Blood vessels uniquely (there is no usual innervation of cholinergic neurons) * Sweat glands similar to eccrine glands effect of the sympathetic nervous system * CNS (in case the agent crosses the BBB) |
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Effects of muscarinic agonists on these parts of the eye (M3)
1) Iris-circular m. 2) ciliary m. 3) lacrimal glands |
1) Miosis (a reduction in pupil size)-contraction
2) Accommodation of focus for near vision (cyclospasm.) 3) Secretion |
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Effects of muscarinic agonists on these parts of the heart (M2)
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Dec. HR (K channel, hyperpolarization)
Dec. AV electrical conduction |
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Effects of muscarinic agonists on Blood Vessels EC (M3)
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Synthesis and release of NO
Vasodilatation |
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Effects of muscarinic agonists on saliva glands (M3)
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Secretion
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Effects of muscarinic agonists on bronchiolar smooth muscle (M3)
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Contracts
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What are the side effects of Anti-muscarinic agents
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Dry mouth, swallowing difficulties
Cycloplegia and mydriasis – Blurred Vision Urinary retention Constipation Dry reddish skin Increased heart rate (tachycardia) Reduced gastric acid secretion “Atropine Fever” –increase in body temperature (specially in children) Hallucinations and confusion |
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What is the treatment for the side effects of Anti-muscarinic agents
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Physostigmine (Assarin)
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Clinical use of muscarinic antagonist
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Diagnostics in Ophthalmology Atropine (Atrospan)
Treatment in GI disorders (Irritable bowl syndrome, IBS)-Spasm in colon and bile– Atropine (Spasmalgin) Asthma Ipratropium Bromide (Aerovent) Treatment of bradycardia (during surgery)- Atropine Incontinence– (no control on urine) Tolterodine (Dertozitol) Treatment for Nerve gas toxicity Atropine+ TMB-4 Toxogonine+ Atropine+Benactizine=TAB |
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effects on the eye of ATROPINE
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Relaxed sphincter muscle of the iris - mydriasis
Relaxed ciliary muscle -cycloplegia |
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Time of effect of Edrophonium
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5-15 min
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Time of effect of Physostigmine
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0.5-2 hrs
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Time of effect of Pyridostigmine
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3-6 hrs
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Indirect cholinergic agonists effects:
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Parasympathetic effects:
Heart- decrease rate Bronchioles- contracts Colon- Inc. activity- secretion Bladder- Increases activity- secretion Sympathetic effects: Sweat glands (Eccrine)- Sweat increase No changes in blood pressure NMJ- Contraction |
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List Reversible - ANTICHOLINESTERASES
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Short Acting: Edrophonium
Med. Acting: - Physostigmine (Eserine) - Neostigmine - Pyridostigmine |
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Drug used to diagnose myasthenia gravis?
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Edrophonium (Tensilon)
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Drug used in TX of myasthenia gravis?
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Pyridostigmine (Mestinon)
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AChE reactivators-OXIMES
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Trimedoxime bromide (TMB-4) =Dipiroxime
Toxogonine = Obidoxime |
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Side effects and overdose effects of these drugs (AChE reactivators-OXIMES)
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Side effects:
Weakness, nausea, Tachycardia, dizziness Overdose: Inhibition of AChE blocks NMJ |
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Nicotine effects
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Increases parasympathetic activities:
Contracts colon Contracts bladder Contracts Bronchioles Increases sympathetic activities: Contracts blood vessels Tachycardia (changes to bradycardia) Skeletal muscles: Increases contraction CNS Increases alertness Stimulation of respiratory system |
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Nicotine toxicity
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Hypertension (blood pressure decreases within a relative short time)
Arrhythmias Convulsions Respiratory interruptions |
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TX of nicotine toxicity
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Artificial respiration
Atropine to reduce the parasympathetic effects Diazepam (Valium) To stop convulsions |
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Effect of Tubocurarine (Currarin)
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NMJ blocker
Effect 1-2 hours Causes histamine release from mast cells |
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Clinical uses of NMJ blockers include:
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1. Easing intubations
2. Relaxing skeletal m. during surgery 3. Easing invasive tests 4. During electroshock therapy to depressive tests, to ease convulsions |
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Drug that inhibits synthesis of noradrenaline
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α-methyltyrosine - Inhibits tyrosine hydroxylase (not in clinical use)
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Drug that inhibits storage of noradrenaline in vesicles
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Reserpine - Inhibits the transporter of neoradrenaline in vesicles
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Catecholamine increase affects:
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In the CNS:
1) Mood (dopamine and NA increase) (cocaine “high”, “rush”) 2) Wakefulness & Concentration 3) Loss of appetite 4) Stimulant (motor & mental) In the Periphery: Inc. levels of NA, causing: 5) Tachycardia, inc. BP 6) Toxicity (O.D.): Cardiac arrhythmias and critical hypertension CNS convulsions |
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Do Amphetamine, Ephedrine, Tyramine and Methylphenidate cross BBB?
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Yes
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What metabolizes Tyramine? (MAO/COMT)
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MAO
NOT COMT |
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What metabolizes amphetamine, ephedrine? (MAO/COMT)
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MAO
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α1 location and mechanism
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SM in blood vessels
Increases IP3 and DAG, which raises Ca concentrations and contractility |
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α2 location and mechanism
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Adrenergic nerves, vasomotor center
Decreases cAMP, which opens K channels, hyperpolarizing the cell |
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β1 location and mechanism
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Cardiac muscle
Increases cAMP, leading to an increase in Ca and contractility |
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β2 location and mechanism
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SM on internal organs
Increases cAMP |
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β3 location and mechanism
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Fat Cells
Inc. cAMP |
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Effects of α1 receptors
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1. Raise blood pressure, due to contraction of smooth muscle on most blood vessels
2. Contract the bladder sphincter to retain urine 3. Dilate pupils (mydriasis) by contracting radial muscle of iris 4. Contract pilomotor muscles on hair follicles |
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Effects of α2 receptors
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1. Inhibit noradrenaline release from presynaptic cells
2. Decrease sympathetic activity 3. Cause contraction of some blood vessels And example of an α2 agonists is Clonidine (α-methyldopa), which is used to treat hypertension and drug withdrawal (for addicts). Side effects include platelet aggregation, inhibition of fat decomposition, inhibition of insulin release, and sweating. |
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Effects of β1 receptors
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1. Increase heart rate and contractility
2. Increase renin release in the kidneys |
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Effects of β2 receptors
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1. Stimulate relaxation of the smooth muscle in the blood vessels, bladder, bronchi, and uterus
2. Increase glycogenolysis and K+ uptake in smooth muscle i. Overactivity may result in a tremor 3. Stimulate glycogenolysis and gluconeogenesis in the liver 4. Stimulate insulin secretion |
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Effects of β3 receptors
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Inc. lipolysis
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Cotransmitters with NE
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ATP
NeuropeptideY-NPY |
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Receptor targeted:Noradrenaline
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α1, α2, β1>>β2
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Receptor targeted: Adrenaline
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α1, α2, β1, β2
clinical use: Prolongation of anesthetic activity |
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Receptor targeted: Isoprenaline
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β1, β2
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Receptor targeted: Pseudoephedrine
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α1, α2
Use: The common cold (runny nose) |
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Receptor targeted: Phenylephrine
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α1>>α2
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Receptor targeted:Clonidine
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α2>>α1
Use: HT |
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Receptor targeted: Salbutamol
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β2>>β1
Use: Asthma |
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Receptor targeted: Dobutamine
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β1>β2
Use; Angina |
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Receptor targeted: Dopamine
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D1, D2>>β>>α
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Adrenergic agonists effect on blood pressure
1) α1 2) β1 3) β2 |
α1: vasoconstriction, inc. TPR, inc. BP
β1: inc. HR, inc SV, inc. CO, inc. BP β2: vasodilation, dec. TPR, dec. BP |
