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MODA Drugs > Pharmacology Of Peripheral Neural Transmission > Flashcards

Pharmacology Of Peripheral Neural Transmission Flashcards

0
Q

Alpha- latrotoxin

A

Spider venom. Acts presynaptically - binds to neurexins (transmembrane proteins on plasma membrane of nerve) to cause the release of neurotransmitters (eg. ACh) via the formation of Ca2+ permeable channels.

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1
Q

AMDA (asymmetric dimethyl arginine)

A

Interfere with L-arginine in the production of NO. Less vasodilatation. High levels associated with cardiovascular diseases. Lowering levels may have important therapeutic effects.

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2
Q

Alpha-methyl dopa

A

Acts as a false transmitter in the place of NA. Acts as an Alpha-2 adrenergic agonist. Less vasoconstriction. Antihypertensive (mainly CNS).

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3
Q

Amitriptyline

A

Serotonin-noradrenaline uptake (1) inhibitor. Tricyclics antidepressant.

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4
Q

Atenolol

A

Beta-1 receptor antagonist. Negative inotropic and chronotropic effect. Treat hypertension, long QT, myocardial infarction.

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5
Q

Atracurium

A

Competitive antagonist of nAChR at NMJ. Block end plate potential and tetanic fade occurs. Skeletal muscle relaxant in anaesthesia.

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6
Q

Atropine

A

Competitive antagonist of mAChR. Parasympatholytic.

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7
Q

Bethanechol

A

Selectively stimulates mAChR without nicotinic. Not selective for subtypes. Parasympathomimetic. Used in bladder dysfunction to stimulate contraction.

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8
Q

Botulinum toxin

A

Binds to SNARE proteins (synaptobrevin, SNAP-25, syntaxin) preferentially on cholingeric neurons. Interfers with release of ACh. Used for excessive sweating, cosmetic, cervical dystonia.

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9
Q

Beta- bungarotoxin

A

Blocks ACh release. Acts through phospholipase A2 and localised to membrane through K+ channel bonding moiety. Causes nerve destruction.

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10
Q

Butaxamine

A

Beta (1) and 2 antagonist. No clinical use.

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11
Q

Caffeine

A

Adenosine 1 receptor antagonist. Relieves drowsiness temporarily. Also inhibits PDE so has +ve chronotropic and inotropic effects. Vasodilator. Diuretic.

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12
Q

Clonidine

A

Slightly selective for alpha 2 adrenergic receptors. Inhibition of SNS output. Antihypertensive.

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13
Q

Clorgiline

A

Selective inhibitor of MAO-A. Prevents degradation of neurotransmitters. Used in depression.

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14
Q

Cocaine

A

Blocks NET uptake 1 transporter.

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15
Q

D-amphetamine

A

Weak inhibitor of MAO. Taken up into vesicle, reduces pH and packaging of amines. Displaced NA leaves nerve ending. Treat ADHD.

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16
Q

Darifenacin

A

mAChR3 antagonist. Decreases bladder contraction. Treat incontinence.

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17
Q

Dipyridamole

A

Blocks adenosine transport back into cells so potentiates responses mediated by adenosine.

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18
Q

Dobutamine

A

Selective B1 agonist. Sympathomimetic. Used in heart failure and acute cardiogenic shock.

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19
Q

D-tubocurarine

A

nAChR antagonist. Not selective for NMJ/ganglion. Skeletal muscle relaxant.

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20
Q

Dyflos

A

Irreversible anti-cholinesterase. Parasympathomimetic. Used to treat glaucoma.

21
Q

Edrophonium

A

Reversible inhibitor of AChE at NMJ. Diagnose myasthenia gravis.

22
Q

Guanethidine

A

Enters nerve by uptake 1, compete with NA. False transmitter. Block release of NA.

23
Q

Hemicholinium

A

Blocks the transporter by which choline is taken up into the nerve. Limits ACh production.

24
Q

Hexamethonium.

A

Use dependent blockade of ganglionic transmission - block of open channel. Used for hypertension. Discontinued due to side effects - loss of para/sympathetic control.

25
Q

Idazoxan

A

Selective A2 antagonist. Possible use as antidepressant/schizophrenia.

26
Q

Imipramine

A

Tricyclic antidepressant. Blocks NET (uptake 1). Increased catecholamine levels.

27
Q

Isoprenaline

A

Non-selective beta agonist. Used in bradycardia, heart block and asthma (old).

28
Q

Labetalol

A

Alpha1/beta antagonist. Used in pregnancy induced hypertension

29
Q

Malathion

A

Long acting, irreversible anticholinesterase. Insecticide to kill lice - paralyse without damaging host.

30
Q

Mecamylamine

A

Nonselective, noncompetitive antagonist of mAChR. Antihypertensive and anti-addictive drug to stop smoking.

31
Q

Muscarine

A

From mushroom. Nonselective agonist of mAChR.

32
Q

Neostigmine

A

Short acting inhibitor of ACherase. Improve muscle tone in myasthenia gravis patients and reverse muscle relaxants.

33
Q

Nicotine

A

Agonist at the ganglionic nAChR, opens ion channel. Long stimulation causes inactivation of VG Na+ channels (phase I block) - depolarising block.

34
Q

Nitroglycerin

A

Nitric oxide donor. Vasodilatation and relaxation of smooth muscle. Angina.

35
Q

Pancuronium

A

Competitive antagonist at nAChR at NMJ. Used in anaesthesia to produce muscle relaxation (fast more than slow).

36
Q

Phentolamine

A

Reversible non selective alpha adrenergic antagonist. Vasodilatation but cause reflex tachycardia and postural hypotension.

37
Q

Phenylephrine

A

Selective a1 agonist. Raise blood pressure in acute hypotension. Decongestant and dilated pupils.

38
Q

Pilocarpine

A

Nonselective muscarinic receptor agonist. Parasympathomimetic. Glaucoma and dry mouth.

39
Q

Pralidoxime

A

Binds to acetylcholinesterase to relieve poisoning from organophosphates. Reverses paralysis of respiratory muscles.

40
Q

Prazosin

A

A1 receptor antagonist. Treat hypertension and anxiety.

41
Q

Propranolol

A

Non selective beta blocker. Hypertension, anxiety and panic.

42
Q

Reserpine

A

Depleted catecholamines from peripheral sympathetic nerve endings by irreversibly blocking VMAT. Neurotransmitters cannot be transported into vesicles.

43
Q

Salbutamol

A

Selective B2 antagonist. Relief of bronchospasm on asthma and COPD.

44
Q

Selegiline

A

MAO-B irreversible inhibitor. Parkinson’s, depression and dementia.

45
Q

Sildenafil

A

Viagra. Inhibits PDE5, reduces degradation of cGMP. Erectile dysfunction and pulmonary arterial hypertension.

46
Q

Suxamethonium

A

Selective for nAChR at NMJ. Block transmission by causing prolonged depolarisation.

47
Q

Tetanus toxin

A

Binds to synaptobrevin. Retrogradely transported back to cell body and then to an inhibitory interneuron - unable to release transmitter so motor neurone more excitable.

48
Q

Tranylcypromine

A

Non selective, irreversible MAO inhibitor. Treatment of refractory depression.

49
Q

Tyramine

A

Indirectly acting sympathomimetic amine. Transported into nerve ending, displaces NA from vesicles and it is released. Only peripherally.

50
Q

Xylazine

A

A2 agonist. Used for anaesthesia and analgesia in animals.

MODA Drugs (5 decks)

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