ANS-CVS 2

Question 1

Example of muscarinic receptors agonist

Answer 1

1. pilocarpine (use as eye drop to treat glaucoma)2. bethanechol

Question 2

Example of muscarinic receptors antagonist

Answer 2

Atropine (treat bradycardia)hyoscine

Question 3

Indirect acting of cholinergic agonist

Answer 3

Action of cholinesterase inhibitors (inhibit Ach catabolism)

Question 4

Types of cholinesterase inhibitors

Answer 4

1. Carbamates (physostigmine, neostigmine)2. Phosphates (isofluorophate)

Question 5

Two type of cholinergic agonist

Answer 5

1. Choline esters (Ach, bethanechol)2. Alkaloids (pilocarpine)

Question 6

What are the effects produced by muscarinic agonists?

Answer 6

Parasympathetic-like effects.1. Smooth muscle (M1) - Increase GI peristaltic activity2. Cardiovascular (M2) - Cardiac slowing, decrease c. output3. Eye (M3) - Contraction of ciliary muscle4. Secretions (M3) - Stimulation of exocrine glands, sweating, lacrimation, salivation and bronchial secretion.

Question 7

what is glaucoma?

Answer 7

increase intraocular pressure due to increase aqueous fluid production and decreased its trabecular outflow.

Question 8

Effects produced by muscarinic antagonists

Answer 8

Sympathetic-like effects1. Smooth muscle (M1) - Bronchial, biliary & urinary tract SM relax. GI transit is inhibited2. Cardiovascular (M2) - Tachycardia3. Eye (M3) - Dilation of the pupil and relaxation of ciliary muscle4. Secrettions (M3) - Inhibition of secretions; dry mouth, bronchial mucociliary clearance is inhibited.

Question 9

Therapeutic uses of muscarinic antagonists

Answer 9

1. GI actions: - treat hyermotility and spasm associated with GI disease (IBS) - Dicycloverine2. Resp. actions: - Treatment of COPD and acute asthma; as bronchodilator - Ipratropium3. Urinary tract: - relieve muscle spasm accompanying infection4. CVS actions: - Treating bradycardia associated with MI - Atropine 5. Overactive bladder: - Reduce spontaneous myocyte activity - decrease frequency and intensity of detrusor activity - M3 receptor antagonists - Adverse reaction - dry mouth, constipation, blurred vision, cardiac arrhythmia

Question 10

Botulinum toxin..

Answer 10

• Botulinum toxin A (BTX-A) most potent and have a longer duration of action- Administered and act in a site specific manner

Question 11

Type of neuromuscular blocking drugs

Answer 11

1. Non depolarising: Block Ach receptors2. Depolarising: Agonists at Ach receptors

Question 12

Examples of competitive antagonists of Ach at mNicotinic receptor:

Answer 12

Tubocurarine analogues1. Mivacurium2. Atracurium3. Vecuronium4. Pancuronium

Question 13

How depolarising agent act as neuromuscular blocking drugs?

Answer 13

• Sustained mNicotinic agonism at NMJ -> depolarisation block

Question 14

Depolarising agent (suxamethonium) is contraindicated in..

Answer 14

1. Neuropathies2. Myopathies (esp malignant hyperthermia)3. Burns/severe trauma (hyperkalaemia -> risk of arrhythmia)

Question 15

Example of AchE inhibitors (indirect cholinergic agonist)

Answer 15

1. Short-acting quaternary alcohols: - e.g. edrophonium - Bind to anionic site -> prevent Ach access - Readily reversible -> brief action - Used in diagnosis of myasthenia gravis2. Medium acting Carbamyl esters - e.g. neostigmine, physostigmine (longer acting) - Carbamyl transfer to anionic site, then slow hydrolysis - As reversal of NMJ block, myasthenia treatment - Also Alzheimer’s (doneprezil, tacrine)3. Irreversible block - e.g. echothiopate (eye drop for glaucoma), dyflos, melathion - Phosphorylate ser203 at active site; stable bond so long lasting - Reversible within first 1-2 hours using pralidoxome

Question 16

Example of direct acting adrenoreceptor agonists

Answer 16

1. dobutamine2. epinephrine3. phenylephrine

Question 17

Example of beta blockers

Answer 17

1. Atenolol2. Propanolol

Question 18

dobutamine

Answer 18

1. direct adrenoceptor agonist2. Effects: - Cardiac stimulation (B1) - Vasodilation (B2)3. clinical use: - cardiogenic shock - acute heart failure - cardiac stimulation during heart surgery4. side effect - arrhythmias

Question 19

epinephrine

Answer 19

1. Effects: - Vasoconstriction and increase BP (a1) - Cardiac stimulation (B1) - Bronchodilation (B2)2. Side effects: - Hypertension - Vasoconstriction - Arrhythmias

Question 20

Example of indirect acting adrenoreceptor agonists

Answer 20

1. amphetamine2. cocaine3. ephedrine

Question 21

cocaine

Answer 21

1. Effects: - Inhibition of norepinephrine reuptake2. Side effects: - hypertension - cardiac damage - necrosis of nasal mucosa (abuse)

Question 22

ephedrine

Answer 22

1. Effects: - vasoconstriction (a1)2. Clinical use - nasal decongestion3. Side effects: - hypertension - tachycardia - insomnia

Question 23

phenylephrine

Answer 23

1. Effects: - Vasoconstriction, increase BP, mydriasis (a1)2. Side effects: - Bradycardia - Hypertension

Question 24

amphetamine

Answer 24

1. Effects: - increase norepinephrine release 2. Side effects: - hypertension - tachycardia - dependence

Question 25

Examples of a-blockers

Answer 25

1. Prazosin 2. Phentolamine

Question 26

prazosin

Answer 26

1. MOA: competitive a1-blocker2. Effects: - vasodilation - decrease vascular resistance and BP - relax bladder neck and prostate3. Clinical use: hypertension4. Side effects: - hypotension - tachycardia - nasal congestion

Question 27

phentolamine

Answer 27

1. MOA: competitive a1 and a2 blocker2. Effects: - Vasodilation - Decrease vascular resistance and BP3. Side effects: - Hypotension - tachycardia - nasal congestion

Question 28

atenolol

Answer 28

1. MOA: B1-blocker2. Effects: - decrease cardiac rate, output, AV node conduction & O2 demand - decrease blood pressure3. Clinical use: hypertension, angina, acute MI, arrhythmia4. Side effects: - Cardiac failure - Bronchoconstriction

Question 29

propanolol

Answer 29

1. MOA: B1 and B2 blocker2. Effects: - decrease cardiac ratem otput, AV node conduction & O2 demand - decrease blood pressure3. Clinical use: hypertension, angina, arrhythmia, acute MI4. Side effects: - cardiac failure - bronchoconstriction

Question 30

Example a & b blockers

Answer 30

Cervedilol

Question 31

carvedilol

Answer 31

1. MOA: - B1 and B2 blocker - a1 blocker2. Effects: - Vasodilation - decrease heart rate and BP in patient with hypertension - increase cardiac output in patient with heart failure