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Pharmacology > Peripheral Neuropharmacology and Acetycholine Agonists > Flashcards

Peripheral Neuropharmacology and Acetycholine Agonists Flashcards

1
Q

Muscarinic receptors - MoA

A

Stimulation leads to activation of G proteins which increase or decrease formation of second messengers

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2
Q

Which muscarinic receptors are coupled with Gq proteins, and what happens when they are activated?

A

M1, M3 and M5. Stimulates Phospholipase C –> Formation of IP3 and diacylglycerol (DAG)

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3
Q

Which muscarinic receptors are coupled with Galpha,i proteins, and what happens when they are activated?

A

M2 and M4. Decreases cAMP levels by inhibiting adenylate cyclase and increases potassium efflux.

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4
Q

Effects of M2 and M3

A

Mioisis, accomodation, lacrimation, mucus secretion, salivation, bronchoconstriction, increased hydrochloric acid secretion, increased motility

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5
Q

Effects of M2

A

Decreased AV conduction and decreased HR

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6
Q

Effects of M3

A

Micturation, erection,

Contracion of smooth muscles and stimulation of glandular secretions. Vasodilation

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7
Q

M1 - Location and MoA

A

Neural (autonomic ganglia, presynaptic nerve terminals and CNS).
Stimulates Phospholipase C –> Increases formation of IP3 and diacylglycerol (DAG)

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8
Q

Effects of M1

A

Modulation of neurotransmission

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9
Q

M2 - Location and MoA

A 
Cardiac tissue (SA and AV node)
Decreases cAMP levels by inhibiting adenylate cyclase and increases potassium efflux.
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10
Q

M3 - Location and MoA

A

Glandular, found in smooth muscle and glands + vascular smooth muscle
Increases IP3 and cGMP as a result of NO stimulation

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11
Q

Nicotinic receptors - Location (type) + MoA

A 
Muscle type (somatic neuromuscular junctions)
Ganglionic type (autonomic ganglia)
CNS type
Activation leads to sodium influx and membrane depolarization --> release of Ca from sarcoplasmic reticulum --> muscle contraction
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12
Q

Muscle type nicotonic receptor - Effects

A

Muscle contracion

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13
Q

Ganglionic and CNS type nicotinc receptor - Effects

A

Excitation of neurons

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14
Q

Direct-Acting Acetylcholine receptor agonists - Groups + synthetic drugs

A

Choline esters
Plant alkaloids
Cevimeline
Varenicline

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15
Q

Choline esters

A

Acethylcholine
Carbachol
Bethanecol

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16
Q

Choline esters - Effects

A

Ocular: Increased lacrimal gland secretion. Stimulates contraction of iris sphincter muscle (miosis) and ciliary muscles (accommodations of lens to focus close objects).

Respiratory: Increased bronchial muscle contraction and mucus secretion.

Cardiac: Decreased impulse formation in SA node by decreasing rate of diastolic depolarization –> slow the heart rate. Slow conduction of cardiac action potential through AV node –> increased PR interval

Vascular: vasodilation(M3 receptor), formation of NO

GI and UT: stimulate salivary, gastric secretion. Increased contraction of GI smooth muscle(Except sphincters) by stim ENS in gut wall –> Increased GI motility.
Stimulate bladder detrusor muscle, promotes emptying of the bladder.

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17
Q

What can high doses of choline esters lead to?

A

Excessive salvation, diarrhea, intestinal cramps and urinary incontinence.

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18
Q

Which choline esters activate both muscarinic and nicotinic receptors?

A

Acetylcholine and Carbachol

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19
Q

What is the name of the choline ester that selectively activates muscarinic receptors?

A

Bethanecol

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20
Q

Acetylcholine - Indication

A

Miosis during ophthalmic surgery
Diagnostic coronary angiography
Diagnose vasospastic angina pectoris

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21
Q

Carbachol - Indication

A

Miosis during ophthalmic surgery

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22
Q

Bethanecol - Indication

A

GI and urinary stimulation. Postop or postpartum to increase bladder muscle tone in pt with nonobstructive neurogenic urinary retention after anesthetics.
Postop adynamic ileus
Atonic stomach (gastroparesis)
Congenital megacolon

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23
Q

Bethanecol - Contraindication

A

IV adm –>leads to hypotension and bradycardia

Obstruction, BPH, PUD, COPD, Ischemic heart disease, Hyperthyroidsm, Parkinson

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24
Q

Plant alkaloids

A

Muscarine
Nicotine
Pilocarpine

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25
Q

Where is muscarine found and what is its adverse effects?

A

Found in toxic mushrooms.

Diarrhea, sweating, salivation and lacrimation

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26
Q

Nicotine - Indication

A

Smoking cessation programs

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27
Q

Pilocarpine - MoA

A

Greater affinity for muscarinic receptor

28
Q

Pilocarpine - Indication

A

2nd line drug for chronic open angle glaucoma and acute angle closure glaucoma (by lowering intraocular pressure)
Xerostomia (by stimulating salivary gland secretion)

29
Q

Pilocarpine - Adverse effects

A

Decreased night vision (caused by miosis)
Difficulty focusing on distal objects (lens accommodates for close vision)
Seizures
CNS damage

30
Q

Cevimeline - MoA

A

Selectively activates M3 receptors

31
Q

Cevimeline - Indication

A

Xerostomia in pt who have had radiation therapy for head/neck cancer
Pt with sjögren syndrome

32
Q

Cevimeline - Adverse effects and Contraindication

A

Increased sweating,
Nausea,
Visual disturbances

Used cautiously in pt with asthma or cardiac arrhythmias

33
Q

Varenicline - MoA

A

Partial agonist at the nicotinic receptor subtype found in the brain that mediates reinforcing effects of nicotine in smokers

34
Q

Varenicline - Indication

A

Smoking cessation

35
Q

Indirect-acting acetylcholine receptor agonist - MoA

A

Affect neurotransmitter synthesis, storage, release or metabolism

36
Q

Edrophonium - MoA

A

Inhibits cholinesterase, preventing the breakdown of acetylcholine at all cholinergic synapses –> rapidly increases acetylcholine concentration

37
Q

Edrophonium - Indication

A

Diagnosis of Myasthenia Gravis
Distinguish between myasthenia crisis and cholinergic crisis in pt treated with cholinesterase inhibitors
Anesthesia (reverse effect of neuromuscular blockade)

38
Q

Physostigmine, Neostigmine and Pyridostigmine - MoA

A

Inh acetylcholinesterase which is responsible for the degradation of acetylcholine

39
Q

Physostigmine - Indication

A

Myasthenia gravis
Reverse seizures and other CNS effects antimuscarinic drugs
Stimulate bladder and bowel
Overdose of atropine, phenothiazine, tricyclic antidepressants

40
Q

Neostigmine - Indication

A 
Myasthenia gravis
Lambert-Eaton syndrome
Diplopia
Blurred vision
Postop urinary retention and abdominal distention
Tubocurarine toxicity
Stimulate bowel and bladder
41
Q

Neostigmine and Pyridostigmine - Adverse effects

A

In case of too high dose: increased muscle weakness due to neuromuscular blockade resulting from excessive ACh

42
Q

Which drugs are used during surgery to reverse the effect of curariform when muscle relaxation is no longer required?

A

Edrophonium
Neostigmine
Pyridostigmine

43
Q

Pyridostigmine - Indication

A

Myasthenia gravis (chronic)
Diplopia
Blurred vision

44
Q

Which drugs are used for Alzheimer disease?

A

Donepezil
Galantamine
Rivastigmine

45
Q

Donepezil, Galantamine, Rivastigmine - MoA

A

Crosses the blood brain barrier and act to increase the concentration of Ach at central cholinergic synapses

46
Q

Echothiophate, Isoflurophate, Malathion - MoA

A

Irreversible acetylcholinesterase inh.

47
Q

Echothiophate - Indication

A

Pesticide
Chronic glaucoma
Stabismus

48
Q

Echothiophate - Adverse effects

A

Organophosphate toxicity

Systemic exposure: effects of muscarinic receptor activation; salivation, lacrimation, miosis, accommodative spasm, bronchoconstriction, intestinal cramps, urinary incontinence

49
Q

Isoflurophate - Indication

A

Chronic glaucoma

50
Q

Malathion - Indication

A

Pesticide, head lice

51
Q

Type 5 phosphodiesterase inhibitors - MoA

A

ACh activates M3 receptors which leads to increased NO –> NO binds to guanylate cyclase and increase synthesis of cGMP. Type 5 phosphodiesterase inhibit breakdown of cGMP leading to increased smooth muscle relaxation –> increased blood flow into penis and erection.

52
Q

Type 5 phosphodiesterase inhibitors - Adverse effects

A

Headache, Nasal congestion, dyspepsia, myalgia, backpain, visual disturbances.
Reduces supine blood pressure(blood pressure when lying on back)

Augments hypotensive effect of vasodilators (alpha-adrenoceptor antagonist) —> used to treat symptoms of urinary obstruction in men with BPH

53
Q

Type 5 phosphodiesterase inhibitors - Contraindication

A

Men who use nitroglycerin or other organic nitrate. Leads to hypotension, reflex tachycardia, worsening of angina pectoris

54
Q

Quasireversible cholinesterase inhibitors

A

Echothiophate
Isoflurophate
Malathion

55
Q

Type 5 phosphodiesterase inhibitors

A

Sildenafil
Tadalafil
Vardenafil
Avanafil

56
Q

Sildenafil - Indication

A

Erectile dysfunction

Pulmonary arterial hypertension

57
Q

Which type 5 phosphodiesterase inhibitor should not be taken with high-fat meal and why?

A

Sildenafil, absorption is reduced

58
Q

Tadalafil - Indication

A

Symptoms of BPH

Pulmonary arterial hypertension

59
Q

Riociguat - MoA

A

Increases cGMP by directly stimulating guanylate cyclase

60
Q

Riociguat - Indication

A

Pulmonary arterial hypertension

61
Q

Riociguat - Contraindication

A

Not use with phosphodiesterase inhibitors due to resulting systemic hypotension

62
Q

Indirect-Acting Acetylcholine Receptor Agonists groups

A 
Reversible cholinesterase inhibitors
Quasireversible cholinesterase inhibitors
Hemicholinium
Vesamicol
Botulinum toxin
Latrotoxin (Black Widow Spider)
63
Q

Reversible cholinesterase inhibitors

A 
Edrophonium
Physostigmine
Neostigmine
Pyridostigmine
Donepezil
Galantamine 
Rivastigmine
64
Q

Hemicholinium - MoA

A

Inhibit choline trasporters which will inhibit Acetylcholine synthesis

65
Q

Vesamicol - MoA

A

Inhibit choline proton transporters on the vesicular membrane, so storage is inhibited

66
Q

Botulinum toxin - MoA

A

Inhibits release of Acetylcholine from vesicles, causes muscle paralysis

67
Q

Latrotoxin (Black Widow Spider) - MoA

A

Release massive amount of Acetylcholine which causes cholinergic crisis

Pharmacology (55 decks)

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