AUTONOMIC DRUGS Flashcards by Shiela Micah Gascon

The parasympathetic preganglionic fibers leave the CNS through
these cranial nerves
A. 1, 5, 9, 10
B. 10, 3, 7, 9
C. 3, 7, 5, 10
D. 2, 7, 10, 5
E. None of the above

ANSWER: B. 10, 3, 7, 9. The parasympathetic preganglionic
fibers leave the CNS through the cranial nerves (CN 3:
Oculomotor, CN 7: Facial, CN 9: Glossopharyngeal, and CN 10:
Vagus).

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The primary receptor type of autonomic ganglia
A. Cholinergic: nicotinic
B. Cholinergic: muscarinic
C. Adrenergic: beta 1
D. Adrenergic: beta 2
E. Dopaminergic: D1-5?

ANSWER: A. Cholinergic: nicotinic.

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Most thoracolumbar preganglionic fibers are?
A. Short
B. Long
C. In networks
D. Connected to organs
E. None of the above

ANSWER: A. Short. Most thoracic and lumbar sympathetic
preganglionic fibers are short and terminate in ganglia located
in the paravertebral chains that lie on either side of the spinal
column. Most of the remaining sympathetic preganglionic fibers
are somewhat longer and terminate in prevertebral ganglia,
which lie in front of the vertebrae, usually on the ventral surface
of the aorta.

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Cholinergic drugs act on receptors normally stimulated by?
A. Norepinephrine
B. Acetylcholine
C. Epinephrine
D. Dopamine
E. None of the above

ANSWER: B. Acetylcholine

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It catalyzes the rate-limiting step in catecholamine biosynthesis
A. L-amino acid decarboxylase
B. Dopamine beta-hydroxylase
C. Phenylethanolamine-N-methyl transferase
D. Tyrosine hydroxylase
E. Dopa decarboxylase

ANSWER: D. Tyrosine hydroxylase catalyzes the rate-limiting
step in the biosynthesis of catecholamines, the conversion of
Tyrosine to Dopa.

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Parasympathetic direct cardiac effects?
A. Decrease heart rate, decrease contractility
B. Increase heart rate, increase contractility
C. Increase AV nodal conduction velocity
D. Decrease heart rate, increase contractility
E. Increase heart rate, decrease contractility

ANSWER: A. Decrease heart rate, decrease contractility

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Drug that prevents the storage of acetylcholine in synaptic
vesicle?
A. Botulinum toxin
B. Vesamicol
C. Metyrosine
D. Tetrodotoxin
E. None of the above

ANSWER: B. Vesamicol. Acetylcholine (ACh) is transported into
the storage vesicle by a vesicle-associated transporter (VAT),
which can be inhibited by vesamicol.

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The rate-limiting step in catecholamine biosynthesis can be
blocked by?
A. Botulinum Toxin
B. Hemicholinium
C. Synaptosomal nerve-associated membrane proteins
D. Metyrosine
E. Vesamicol

ANSWER: D. Metyrosine.
see figure

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The acetylcholine vesicle release process can be blocked by?
A. Hemicholinium
B. Vesamicol
C. Botulinum toxin
D. Vesicle-associated membrane proteins
E. Synaptosomal nerve-associated membrane proteins

ANSWER: C. Botulinum toxin. The resulting increase in
intracellular calcium causes fusion of vesicles with the surface
membrane and exocytotic expulsion of acetylcholine and
cotransmitters into the junctional cleft. This step can be blocked
by botulinum toxin.

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In the cytoplasm, acetylcholine is synthesized from choline and
Acetyl-CoA by what enzymes?
A. Acetylcholinesterase
B. Choline acetyltransferase
C. Vesicle associated transporter
D. Phenylethanolamine-N-methyltransferase
E. None of the above

ANSWER: B. Choline acetyltransferase. Acetylcholine (ACh) is
synthesized in the cytoplasm from acetyl-CoA and choline
through the catalytic action of the enzyme choline
acetyltransferase (ChAT).

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This drug can block the reuptake of noradrenergic transmitters
into the nerve terminal
A. Reserpine
B. Cocaine
C. Guanethidine
D. Metyrosine
E. Bretylium

ANSWER: B. Cocaine. NET can be inhibited by cocaine and
certain antidepressant drugs, resulting in an increase of
norepinephrine activity in the synaptic cleft.

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Rate limiting step in acetylcholine synthesis
A. Availability of acetate
B. Choline acetate activity
C. Choline uptake
D. Vesicular protein synthesis
E. Acetylcholinesterase activity

ANSWER: A. Availability of acetate

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Inhibits choline transfer into cholinergic vesicles
A. Atropine
B. Bretylium
C. Reserpine
D. Vesamicol
E. All of the above

ANSWER: D. Vesamicol

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Influx of this ion promotes fusion between axoplasmic
membrane and nearby vesicles
A. Potassium
B. Chloride
C. Calcium
D. Sodium
E. All of the above

ANSWER: C. Calcium. Release of transmitters occurs when
voltage-sensitive calcium channels in the terminal membrane
are opened, allowing an influx of calcium. The resulting increase
in intracellular calcium causes fusion of vesicles with the surface
membrane and exocytotic expulsion of acetylcholine and cotransmitters into the junctional (synaptic) cleft.

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Which is not a choline ester?
A. Arecoline
B. Acetylcholine
C. Bethanechol
D. Carbachol
E. Methacholine

ANSWER: A. Arecoline. Acetylcholine and methacholine are
acetic acid esters of choline and β-methylcholine, respectively.
Carbachol and bethanechol are carbamic acid esters of the same
alcohols.

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Which among the following choline ester drugs is the most
susceptible to hydrolysis by the enzyme cholinesterase?
A. Arecoline
B. Carbachol
C. Acetylcholine
D. Metacholine
E. Bethanecol

ANSWER: C. Acetylcholine.

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Which among the following choline ester drugs has the most
muscarinic action?
A. Acetylcholine
B. Bethanecol
C. Carbachol
D. Methacholine
E. Arecoline

ANSWER: D. Methacholine. See above table.

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This direct-acting cholinomimetic drug is used for postoperative
ileus and urinary retention?
A. Pilocarpine
B. Carbachol
C. Arecoline
D. Bethanecol
E. Nicotine

ANSWER: Bethanecol

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Effects of direct-acting cholinoceptor stimulants except?
A. Sinoatrial node: positive chronotropy
B. Bronchial muscles: bronchoconstriction
C. Sphincter muscle of iris: miosis
D. Gastrointestinal tract motility: increase
E. All are correct

ANSWER: A. Sinoatrial node: positive chronotropy

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The ff are indirect acting cholinomimetic drugs except
A. Acetylcholine
B. Neostigmine
C. Echothiophate
D. Edrophonium
E. Carbaryl

ANSWER: A. Acetylcholine is a direct-acting cholinomimetic
drug.

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The following are effects of anticholinesterase except?
A. Miosis
B. Bradycardia
C. Reduced muscle contraction
D. Hypersalivation
E. All are correct

ANSWER: C. Reduced muscle contraction. Anticholinesterases
aka cholinesterase inhibitors block the degradation of
acetylcholine and thereby prolong its action. Because the
primary action is to amplify the actions of endogenous
acetylcholine, the effects are similar (but not always identical)
to the effects of the direct-acting cholinomimetic agonists.

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Long-term therapy for myasthenia gravis is usually
accomplished with?
A. Pyridostigmine
B. Physostigmine
C. Neostigmine
D. Edrophonium
E. Echothiophate

ANSWER: A. Pyridostigmine. Edrophonium is for acute
treatment only. While both pyridostigmine and neostigmine are
both used for treatment of myasthenia gravis, pyridostigmine
has a longer duration of action (4-6 hours).

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This anticholinesterase organophosphate drug was used as an
ophthalmic solution for treating glaucoma?
A. Neostigmine
B. Echothiophate
C. Edrophonium
D. Physostigmine
E. Pyridostigmine

ANSWER: B. Echothiophate. See above table.

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Which of the following reversible cholinesterase inhibitor is not
used in the treatment of myasthenia gravis?
A. Physostigmine
B. Pyridostigmine
C. Neostigmine
D. Edrophonium
E. All drugs can be used

ANSWER: A. Physostigmine is used for anticholinergic
poisoning. Refer to #23 table.

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25. Anticholinesterase used for atropine intoxication A. Neostigmine B. Physostigmine C. Pyridostigmine D. Echothiophate E. NOTA

ANSWER: B. Physostigmine is used for anticholinergic poisoning

26. Effect of Atropine on the heart? A. Tachycardia B. Bradycardia C. Hypercapnia D. Bradyarrhythmia E. No effect on the heart

ANSWER: A. Tachycardia. Atropine will increase the heart rate.

27. Atropine is previously used prior to general anesthesia to reduce A. Nausea and vomiting B. Muscle tone C. Oral secretions D. Anxiety E. All of the above

ANSWER: C. Oral secretions. The use of atropine became part of routine preoperative medication when anesthetics such as ether were used, because these irritant anesthetics markedly increased airway secretions and were associated with frequent episodes of laryngospasm. Preanesthetic injection of atropine or scopolamine could prevent these hazardous effects.

28. Which of the following antimuscarinic drug is often effective in preventing or reversing vestibular disturbances especially motion sickness? A. Homatropine B. Atropine C. Benztropine D. Tropicamide E. Scopolamine

ANSWER: E. Scopolamine. Certain vestibular disorders respond to antimuscarinic drugs (and to antihistaminic agents with antimuscarinic effects). Scopolamine is one of the oldest remedies for seasickness and is as effective as any more recently introduced agent.

29. The following are clinical uses of muscarinic blocking drugs except? A. Parkinson’s disease B. Hypertension C. COPD D. Hypermotility E. Prevention of synechia

ANSWER: B. Hypertension. The sinoatrial node is very sensitive to muscarinic receptor blockade. Moderate to high therapeutic doses of atropine cause tachycardia in the innervated and spontaneously beating heart by blockade of vagal slowing.

30. Oxybutynin that is used to relieve bladder spasm after prostatectomy, is somewhat selective to what specific receptor? A. M1 B. M2 C. M3 D. M4 and M5 E. AOTA

ANSWER: C. M3

31. The prototype drug for parasympatholytic group is? A. Homatropine B. Atropine C. Scopolamine D. Dicyclomine E. Glycopyrrolate

ANSWER: B. Atropine

32. The definitive treatment for organophosphate poisoning is? A. Atropine B. Ipratropium C. Physostigmine D. None of the above

ANSWER: A. Atropine. Treatment: 1–2 mg of Atropine sulfate may be given intravenously every 5–15 minutes until signs of effect (dry mouth, reversal of miosis) appear.

33. Primary effects of muscarinic blocking agents except A. Miosis B. Bronchodilation C. Decreased salivary secretion D. Increased heart rate E. Mydriasis

ANSWER: A. Miosis. The primary effect in the eye is mydriasis (dilation).

34. This drug directly interacts with and activate adrenoreceptors A. Tricyclic antidepressants B. Tyramine C. Epinephrine D. Cocaine E. COMT inhibitors

ANSWER: C. Epinephrine

36. This drug induces the release of catecholamines by displacing them from adrenergic nerve endings A. Monoamine oxidase inhibitors B. Tyramine C. Tricyclic antidepressants D. Cocaine E. Norepinephrine

ANSWER: B. Tyramine. Induce release of catecholamines by displacing them from adrenergic nerve endings is the mechanism of action of Tyramine.

37. Vasopressor of first choice in the management of shock? A. Dopamine drip B. Epinephrine C. Norepinephrine drip D. Dobutamine drip

ANSWER: C. Norepinephrine.

38. Alpha 2 receptor agonist that is used in the treatment of hypertensive emergency? A. Clonidine B. Oxycarbamazine C. Ipratropium D. Dobutamine E. Phenylephrine

ANSWER: A. Clonidine. Clonidine, Methyldopa (for pregnant with high bp), Guanfacine and Guanabenz are useful in the treatment of hypertension. Dobutamine is used as a pharmacologic cardiac stress test. Phenylephrine increases BP without increasing heart rate. Ipratropium is an anticholinergic drug

39. Adverse effects from using phenoxybenzamine includes all of the following except: A. Inhibition of ejaculation B. Bradycardia C. Orthostatic hypotension D. Nasal stuffiness E. Sedation

ANSWER: B. Bradycardia. Adverse effects of Phenoxybenzamine: (a) Orthostatic hypotension and Tachycardia (b) Nasal stuffiness and inhibition of ejaculation (c) Enters the CNS – may cause fatigue, sedation and nausea.

40. Which of the following alpha receptor blocker does not dissociate from receptors and the block cannot be surmounted with sufficiently high concentrations of agonists? A. Labetalol B. Phentolamine C. Phenoxybenzamine D. Prazosin E. All of the above

ANSWER: C. Phenoxybenzamine. Phenoxybenzamine is an irreversible drug that do not dissociate and cannot be surmounted. Phentolamine and Prazosin are reversible antagonists that dissociate from receptors and the block can be surmounted with sufficiently high concentrations of agonists. Labetalol is a beta-receptor blocker

41. Selective alpha antagonist like prazosin, terazosin, alfuzosin and tamsulosin are indicated in? A. Benign prostatic hyperplasia B. Hypertensive emergencies C. Pheochromocytoma D. Erectile dysfunction E. All of the above

ANSWER: A. Benign Prostatic Hyperplasia (BPH)

42. An alpha-adrenoceptor antagonist that was used in the treatment of male erectile dysfunction is? A. Phentolamine B. Prazosin C. Yohimbine D. Labetalol E. None of the above

OTHERTERM- SILDENAFIL ANSWER: C. Yohimbine. Treat male erectile dysfunction but has been superseded by phosphodiesterase-5 inhibitors like

42. An alpha-adrenoceptor antagonist that was used in the treatment of male erectile dysfunction is? A. Phentolamine B. Prazosin C. Yohimbine D. Labetalol E. None of the above

ANSWER: C. Yohimbine. Treat male erectile dysfunction but has been superseded by phosphodiesterase-5 inhibitors like sildenafil.

43. An ultra-short-acting beta 1-selective adrenoreceptor antagonist that is rapidly metabolized by esterases in red blood cell A. Esmolol B. Atenolol C. Nadolol D. Timolol E. None of the Above

ANSWER: A. Esmolol. Ultra-short-acting beta 1-selective adrenoceptor antagonist. Esterases in red blood cells rapidly metabolize esmolol to a metabolite that has a low affinity for beta receptors. Metoprolol and Atenolol preferable in patients with diabetes or peripheral vascular disease when therapy with a beta blocker is required. Nadolol has a very long duration of action. Timolol has excellent ocular hypotensive effects when administered topically in the eye.

44. Immediate precursor in the synthesis of noradrenaline? A. Midodrine B. Adrenaline C. Epinephrine D. Dopamine

ANSWER: D. Dopamine. Tyrosine is converted to dopamine and transported into the vesicle by VMAT, which can be blocked by reserpine and tetrabenzine. Dopamine is converted to norepinephrine in the vesicle by dopamine-beta-hydroxylase.

45. Most highly selective beta 1-adrenergic receptor blocker? A. Timolol B. Nadolol C. Nebivolol D. Labetalol E. Carvedilol

ANSWER: C. Nebivolol.

46. Beta-receptor antagonist drug with the longest duration of action? A. Levobunolol B. Betaxolol C. Metoprolol D. Atenolol E. Nadolol

ANSWER: Nadolol

47. Propranolol, which is a beta 1 and 2 adrenoceptor antagonist, is indicated for the ff diseases except: A. Migraine B. Glaucoma C. Arrythmia D. Bronchial asthma E. Angina pectoris

ANSWER: D. Bronchial asthma

48. The following are beta 1 selective antagonist except? A. Timolol B. Esmolol C. Propranolol D. Atenolol E. All of the above is correct

ANSWER: A. Timolol / C. Propranolol both has no selectivity.

49. The prototype beta-receptor antagonist drug? A. Metoprolol B. Atenolol C. Timolol D. Propranolol E. Nadolol

ANSWER: D. Propranolol

50. Preferred beta blocker drug for patients with diabetes or peripheral vascular disease A. Propranolol B. Esmolol C. Metoprolol D. Nadolol E. None of the above

ANSWER: C. Metoprolol. Metoprolol and Atenolol preferable in patients with diabetes or peripheral vascular disease when therapy with a beta blocker is required.

51. The primary transmitter at ANS ganglia, at the somatic neurons

ANSWER: Acetylcholine

52. The primary transmitter at most sympathetic postganglionic neurons

ANSWER: Norepinephrine

Sympathetic Nervous System – originates from thoracolumbar

(Thoracic 1-T12 and L1-L2)

Parasympathetic – originates from Craniosacral

(CN 3- Oculomotor, CN 7- Facial, CN 9- Glossopharyngeal, CN 10- Vagus)

Five Key Features of Neurotransmitter Function

(SSR-TR) 1. SYNTHESIS 2.STORAGE 3.RELEASE 4.TERMINATION OF ACTION OF THE TRANSMITTER 5.RECEPTOR EFFECTS

There are two types of transmission:

1.CHOLINERGIC TRANSMISSION 2.ADRENERGIC TRANSMISSION

involves the transmission of Acetylcholine

CHOLINERGIC TRANSMISSION

involves release of Norepinephrine/Noradrenaline

ADRENERGIC TRANSMISSION

WHAT TYPE OF TRANSMISSION Choline is transported into the cytoplasm at the terminal button by a sodium-dependent choline transporter (CHT). This symporter can be blocked by research drugs called ___

CHOLINERGIC TRANSMISSION HEMICHOLINIUMS

Once the acetylcholine is formed, it must be stored inside a vesicle by a vesicle-associated transporter (VAT).

inhibited by VESAMICOL

inhibit the release of stored choline

BOTULINUM TOXIN

Once the acetylcholine is released in the synaptic cleft, it will be degraded by____ and others would bind on cholinergic receptors and others will go back into the nerve by the acetylcholine autoreceptors.

acetylcholinesterase (AChE)

Tyrosine is transported into the noradrenergic nerve ending by a sodium-dependent carrier.

ADRENERGIC TRANSMISSION

Tyrosine is converted to dopamine by the rate limiting enzyme ____ and it can be blocked by ____

Tyrosine is converted to dopamine by the rate limiting enzyme **tyrosine hydroxylase** and it can be blocked by **metyrosine**

From dopamine it will converted into norepinephrine by _______ and transported into the vesicle by the vesicular monoamine transporter (VMAT), which can be blocked by ______ and _____. The same carrier transports norepinephrine (NE) and several related amines into these vesicles.

---dopamine β-hydroxylase ---blocked by reserpine and tetrabenazine.

which blocks the vesicular monoamine transporter (VMAT)

RESERPINE TETRABENZINE

rate limiting enzyme in the convertion if tyrosine to dopamine

TYROSINE HYDROXYLASE

in adrenergic transmission After release, norepinephrine diffuses out of the cleft or is transported into the cytoplasm of the terminal by the norepinephrine transporter (NET), which can be blocked by ___________ and ____________

COCAINE DEPRESSANTS

CHOLINOCEPTOR

1. MUSCARINIC 2. NICOTINIC

ADRENOCEPTOR

1. alpha adrenoceptor 2. beta adrenoceptor 3. dopamine receptor

Bind to and activate muscarinic or nicotinic receptors.

DIRECT-ACTING CHOLINOMIMETIC DRUGS

- Produce their primary effects by inhibiting acetylcholinesterase, which hydrolyzes acetylcholine to choline and acetic acid. - there will be an increase in the concentration of acetylcholine receptors in the synaptic cleft

INDIRECT-ACTING CHOLINOMIMETIC DRUGS

SUSCEPTIBILITY TO CHOLINESTERASE 1. Acetylcholine chloride 2. Methacholine chloride

SUSCEPTIBILITY TO CHOLINESTERASE 1. Acetylcholine chloride. ++++ 2. Methacholine chloride +

MUSCARINIC ACTION 1. Acetylcholine chloride 2. Methacholine chloride

MUSCARINIC ACTION 1. Acetylcholine chloride +++ 2. Methacholine chloride ++++ —In Methacholine chloride it is mostly in the muscarinic receptor that it will activate.

NICOTINIC ACTION 1. Acetylcholine chloride 2. Methacholine chloride

NICOTINIC ACTION 1. Acetylcholine chloride +++ 2. Methacholine chloride none

When you inject acetylcholine in patients, the heart rate and the contraction of the heart will ____. increase or decrease?

DECREASE

When you inject acetylcholine in your patients what happens to the bronchial glands?

+there will be SECRETION

The antidote for acetylcholine overdose is _____. and will ____ the heart rate. (increase or decrease)

ATROPINE -INCREASE

used as a diagnostic test for myasthenia gravis

EDROPHONIUM

MYASTHENIA GRAVIS TREATMENT

1. NEOSTIGMINE 2. PYRIDOSTIGMINE

Organic derivatives of phosphoric acid

ECHOTHIOPHATE

In GLAUCOMA, the optic nerve is damaged due to increase intraocular pressure in the eyes. The normal intraocular pressure is 10-21 mmHg. VASODILATION 1. relieve ICP 2. decrease formation of aqeous humor 3. contract ciliary body to have outflow of aqeous humor

ECHOTHIOPHATE

CHOLINOMIMETICS

• Treat diseases of the eye (glaucoma, accommodative esotropia) In glaucoma, the optic nerve is damaged due to increase intraocular pressure in the eyes. The normal intraocular pressure is 10-21 mmHg. • Gastrointestinal and urinary tracts (postoperative atony, neurogenic bladder) • Neuromuscular junction (myasthenia gravis, curare- induced neuromuscular paralysis) • Treat patients with Alzheimer’s disease • Treatment of Atropine overdosage • Atrial arrhythmias (rare)

decrease in ACETYLCHOLINE to increase it give CHOLINOMIMETICS

ALZHEIMERS DISEASE

Smoking cessation Insecticides

Nicotine

Post operative and neurogenic ileum Urinary retention

Bethanechol

GlaucOma sjogrens syndrome

Pilocarpine

(C-A-P) CNS neurons, autonomic postganglionic cell bodies presynaptic sites

M1 RECEPTOR SUBTYPE

(M-S) Myocardium smooth muscle organs

M2 RECEPTORS

Effector cell membranes - glandular - smooth muscle cells

M3 RECEPTORS

Î in CNS than Periphery

M4 & M5 RECEPTORS

They block the effects of parasympathetic autonomic discharge ( acetylcholine )

Muscarinic Antagonists Antimuscarinic Parasympatholytic

Prototype

Atropine

For asthma COPD Î airway

Tiotropium

↓ lackimation

Glycopyprolate

Mydriatic Cycloplegic

Tropicamide

Peptic disease Hypermotility

Dicyclomine

Î acetylcholine ↓ dopamine

Parkinson's disease

Combination of an antimuscarinic agent with a dopamine precursor drug (LEVODOPA) provide an effective therapy

PARKINSONS DISEASE

− Involve muscarinic cholinergic transmission − Antimuscarinic drugs

MOTION SICKNESS

treatment for Motion sickness

SCOPOLAMINE

____ greatly facilitates ophthalmoscopic examination of the retina -Antimuscarinic agents (topically as eye drops or ointment) -Prevent synechia (adhesion) formation in uveitis and iritis

MYDRIASIS

CARDIOVASCULAR DISORDERS a. Vasovagal attack (give __ to increase the heart rate) b. Hyperactive carotid sinus reflexes c. Graves’ disease (hyperthyroidism) also have such antibodies that may facilitate the development of atrial fibrillation.

ATROPINE r related antimuscarinic agent

COPD

(A-T-I-U) x -IUM ACLIDINIUM TIOTROPIUM IPRATROPIUM UMECLIDINIUM

GASTROINTESTINAL DISORDERS a. Peptic Ulcer Disease b. Common traveler’s diarrhea c. Other mild or self-limited conditions of hypermotility

Atropine + diphenoxylate (LOMOTIL)

Bladder spasm after urologic surgery (prostatectomy)

OXYBUTYNIN (M3 RECEPTOR)

Urinary incontinence

Propiverine (anti-muscarinic)

Benign Prostatic Hyperplasia

α-adrenoceptor antagonist combined with a muscarinic antagonist

CHOLINERGIC POISONING a. Cholinesterase inhibitor insecticides b. Chemical warfare “nerve gases” c. Organophosphorus poisoning

ATROPINE SULFATE 1–2 mg of Atropine sulfate INTRAVENOUSLY every 5–15 minutes until signs of effect ( dry mouth, reversal of miosis) appear.

Organophosphate poisoning and insecticide poisoning are treated with antimuscarinic drugs. ○ In insecticide poisoning, there is low heart rate, increased secretions, miotic, breathing problems due to bronchial secretions, and increased bronchial activity.

CHOLINERGIC POISONING