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Deck of Secret Knowledge > Pharm: Autonomic Drugs > Flashcards

Pharm: Autonomic Drugs Flashcards

0
Q

Botulinum toxin inhibits which particular SNARE protein?

A

T SNARE, synaptobrevin

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1
Q

What is the neurotransmitter at the sympathetic postganglionic neurons to the thermoregulatory sweat glands?

A

Acetylcholine

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2
Q

What 2 organs have Ach at their post ganglionic sympathetic synapse?

A

Thermoregulatory eccrine sweat glands AND vasodilatory sympathetic nerve fibers in the skeletal muscle.

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3
Q

Which transporter transports norepinephrine and dopamine into vesicles where they are stored? Which inhibits these transporters?

A

Vesicular monoamine transporter

Reserpine

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4
Q

This drug blocks release of norepinephrine from vesicles

A

Guanethidine

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5
Q

These drugs promote catecholamine release

A

Amphetamines

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6
Q

Release of renin is stimulated by action of catecholamines on which receptors.

A

Beta 1

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7
Q

Which 2 direct acting cholinomimetics are useful for BOTH muscarinic and nicotinic receptors?

A

Acetylcholine and carbachol

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8
Q

Which is a muscarinic cholinomimetic that has GOOD lipid solubility?

A

ONLY Pilocarpine.

Acetylcholine carbs hop and bethenachol all fulfill the the criteria EXCEPT for lipid solubility.

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9
Q

What is an example of an M1 selective anti muscarinic?

A

Pirenzipine ad tirenzipine

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10
Q

Which adrenergic receptor is found in the liver?

A

Beta 2. Increase with glycogenolysis

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11
Q

Where is the dopamine 1 receptor located and what is its function?

A

Smooth muscle.

Relax renal vascular smooth muscle

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12
Q

Is the myenteric plexus activated or inhibited by the parasympathetic system? On which receptors does acetylcholine act on?

A

Activates.

M1

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13
Q

What is the action of the SNS on:

  1. Pilomotor smooth muscles
  2. Thermoregulatory sweat glands
  3. Apocrine (sweat) glands
A
  1. Contracts (alpha)
  2. Activates (M; acetylcholine)
  3. Activates (alpha)
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14
Q

Acts on nerve terminal Ca channels and prevent transmitter release

A

Conotoxin

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15
Q

Inhibit uptake of adrenergic neurotransmitter a prolonging effect on postsynaptic receptors

A

Cocaine

TCA

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16
Q

What is the predominant autonomic tone in the:

  1. Heart
  2. Blood vessels
A
  1. Parasympathetic

2. Sympathetic

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17
Q

Which inhibits breakdown of adrenergic neurotransmitters at the nerve terminal?

A

Monoamine oxidase

Tranylcypromine

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18
Q

Nicotinic agonist with partial agonist properties; reduces craving in persons addicted to nicotine

A

Varenicline

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19
Q

This cholinesterase inhibitor is exclusively used in Alzheimer’s disease

A

Rivastigmine

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20
Q

Name two organophosphates used in medicine and their indications

A

Malathion - scabicide

Metrifonate - antihelminthic

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21
Q

How does edrophonium differentiate between myasthenic crisis and cholinergic crisis?

A

Improves strength in myasthenic crisis; weakens it in cholinergic crisis

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22
Q

T/F. Atropine, the antidote in organophosphate poisoning, effectively decreases nicotinic signs of toxicity.

A

False. Atropine acts on muscarinic receptors. Nicotinic toxicity is treated by regenerating active cholinesterase.

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23
Q

Direct acting muscarinic agonist used in bladder and bowel atony

A

Bethanechol

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24
Q

Nicotinic receptor agonist used for muscle relaxation. With prolonged action in px with abnormal butylcholinesterase

A

Succinylcholine

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25
Q

What inhibits the rate limiting step in adrenergic transmission using NE?

A

Metyrosine. The conversion of TYR to Dopa accomplished by tyrosine hydroxylase is the rate limiting step.

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26
Q

Give the noradrenergic system equivalent of: Hemicholinium, vesamicol and botulinum

A

Metyrosine, reserpine and guanethedine

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27
Q

Rate limiting step in the synthesis of acetylcholine.

Which experimental drug inhibits this step?

A

Transport of choline into the nerve terminal.

Hemicholinium

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28
Q

This drug inhibits transport of acetylcholine into vesicles by vesicle-associated transporter.

A

Vesamicol

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29
Q

Most dangerous effect of atropine toxicity in children

A

“Atropine fever”

Blockade of thermoregulatory sweating

30
Q

Nicotinic ganglion blocker that enters the CNS and has shown benefit in smoking cessation and amelioration of Tourette’s syndrome

A

Mecamylamine

31
Q

Nonselectice anti muscarinic drug used in incontinence and urinary urgency

A

Oxybutynin

32
Q

Anti-muscarinic used in motion sickness

A

Scopolamine

33
Q

Anti muscarinic drug used in COPD

A

Tiotropium

34
Q

Platelets have which type of adrenergic receptor. Activation of this receptor would lead to which action.

A

Alpha-2

Platelet aggregation

35
Q

This drug of abuse promotes release of adrenergic neurotransmitters while another drug of abuse prevents its reuptake

A

Amphetamine promotes release

Cocaine prevents reuptake

36
Q

Name 2 alpha-2 selective antagonists

A

Yohimbine

Rauwolscine

37
Q

Name 2 non selective alpha blockers

A

Phenoxybenzamine

Phentolamine

39
Q

These beta blockers are in fact partial agonists and in theory may be beneficial in patients with asthma.

A

Pindolol
Acebutolol

Pwede sa Asthma (Pindolol, Acebutolol)

39
Q

What is the longest acting beta blocker?

A

Nadolol

40
Q

Besides its use in pheochromocytoma what conditions may also be remedied by phenoxybenzamine?

A

Carcinoid and mastocytosis

41
Q

Nonselective beta blockers lacking anesthetic action; useful in glaucoma

A

Timolol

Betaxolol

42
Q

What is the effect of sympathetic stimulation on insulin function

A

Alpha 2 activation leads to inhibition of insulin release

Beta 2 activations leads to insulin release

43
Q

Beta 3 receptors are found on which cells? Activation leads to __

A

Fat cells

Lipolysis

44
Q

Clonidine is sometimes given in hypertension. What is its mechanism of action?

A

It is an alpha 2 agonist, accumulates in the CNS and reduce sympathetic outflow and BP.

45
Q

What drug do you use for pheochromocytoma patients preoperatively? During surgery?

A

Phenoxybenzamine used pre-op; with long duration of action (24-48h).
Phentolamine used during surgery.

46
Q

Indications for use of phenoxybenzamine

A

Pheochromocytoma
Carcinoid
Mastocytosis
Raynaud’s Phenomenon

47
Q

Name b1-selective beta blockers.

A

Atenolol
Esmolol
Metoprolol

48
Q

Beta blocker used for perioperative and thyroid storm arrhythmia and hypertensive emergencies

A

Esmolol

49
Q

Name 2 drugs that block both alpha and beta receptors

A

Labetalol
Carvedilol

Both with mortality benefit in heart failure.

50
Q

Name one b2-selective blocker.

A

Butoxamine

51
Q

This drug is used in Cushing’s disease and reduces catecholamine levels by inhibiting tyrosine hydroxylase.

A

Metyrosine

52
Q

Peripheral dopamine hydroxylase inhibitor given along with L-DOPA in the treatment of Parkinson’s disease

A

Carbidopa

53
Q

This local anesthetic impairs reuptake of catecholamine transmitters.

A

Cocaine

54
Q

Differentiate hemicholinium from hexamethonium.

A

Hemicholinium - inhibit transport of choline into cholinergic nerve endings
Hexamethonium - research drug that blocks all ANS ganglia

55
Q

T/F. Vagal stimulation and administration of cholinomimetic agents cause bradycardia.

A

False!

Vagal stimulation causes bradycardia. Cholinomimetic agents, on the other hand, cause vasodilation (by releasing EDRF) and subsequent reflex tachycardia.

56
Q

3/M eats a mushroom and experiences nausea, vomiting and diarrhea. What is responsible for this reaction?

A

Muscarine and alkaloids in certain mushrooms cause muscarinic toxicity

57
Q

Only a few organosphosphates are used in medicine:

  1. Antihelminthic agent
  2. Scabicide
A
  1. Metrifonate

2. Malathion

58
Q

Atropine is used for muscarinic toxicity. What is the antidote for nictonitic toxicity?

A

Pralidoxime inhibits anticholinesterase inhibitors; and are effective in both muscarinic and nicotinic toxicity.

59
Q

Indirect acting cholinomimetics

  1. Reversal of severe atropine poisoning
  2. Alzheimer’s disease
  3. Treatment of MG
A
  1. Physostigmine
    PHysostigmine PHixes atropine toxicity.
  2. Rivastigmine, galantamine, donepezil
  3. Pyridostigmine
60
Q

Many muscarine antagonists are nonselective except ____ which is selective for M1. What is a current indication for its use?

A

Pirenzepine.

Peptic ulcer

61
Q

Two smoking cessation agents act on cholinergic transmission.

  1. Partial muscarinic agonist
  2. Nicotinic ganglion blocker
A
  1. Varenicline

2. Mecamylamine

62
Q

This ganglion-blocking drug may ameliorate symptoms of Tourette’s syndrome.

A

Mecamylamine

63
Q

Which antimuscarinic is indicated in the following conditions:

  1. COPD
  2. Motion sickness
  3. Ophthalmic use to produce mydriasis
  4. Incontinence
A
  1. Tiotropium, ipratropium
  2. Scopolamine
  3. Atropine, homatropine, cyclotropine, tropicamide
    (EYE’M At Home when the Cyclone hit the Tropics)
  4. Oxybutinin
64
Q

Explain how the different autonomic drug classes can help reduce IOP in glaucoma.

  1. Beta blocker
  2. A2-agonist
  3. Muscarinic agonist
  4. Anticholinesterase inhibitor
  5. Alpha nonselective
A

1 and 2 decrease aqueous humor production (“turn the tap off”). Examples include timolol and carteolol (beta blockers); and brimonidine and apraclonidine (a2-agonist).

3 and 4 increase outflow of aqueous humor (“unclog the drain”) by contracting the ciliary muscle and pulling on the trabecular meshwork. Examples include pilocarpine and carbachol (cholinomimetic) and physostigmine (AChe inhibitor.)

5 increases aqueous outflow via uveoscleral veins

65
Q

Clonidine decreases the blood pressure. T/F.

A

Not always!

IV/intranasal clonidine increases BP.

66
Q

Activation of the following beta hormones increase release of which hormones.

  1. Beta 1
  2. Beta 2
A
  1. Renin

2. Insulin

67
Q

Autonomic drug used in the treatment of attention deficit disorder

A

Methylphenidate

Amphetamine analog

68
Q

The effects of all alpha-antagonists except this drug can be surmounted by increased concentration of agonist.

A

Phenoxybenzamine

Produces an irreversible block

69
Q

What is epinephrine reversal? This effect is not seen with phenylephrine or norepinephrine. Why?

A

Epinephrine reversal describes the reversal of BP effect of large doses of epinephrine from a pressor response (alpha) to a depressor response (beta 2); after administration of an alpha blocker. This is NOT seen with phenylephrine or norepinephrine because these drugs lack sufficient B2 effects.

70
Q

This alpha-2 selective blocker is used in the treatment of depression.

A

Mirtazapine

71
Q

This beta two agonist is used to reduce premature uterine contractions. It acts on which receptor subtype.

A

Ritodrine

B2-selective blocker

72
Q

Guanethedine becomes inactive because this drug inhibits its transport into nerve terminals.

A

TCA / cocaine

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