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Term 1 MD > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Acetylcholine

A

Muscarinic and nicotinic agonist
Use: To obtain miosis after delivery of the lens in cataract surgery and other procedures where rapid miosis (eye constriction) is required

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2
Q

Methacholine

A

Muscarinic agonist
Use: Diagnosis of bronchial airway hyperreactivity in subjects who do not have clinically apparent asthma

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3
Q

Bethanechol

A

Muscarinic agonist
Use: Post-operative urinary retention and atony of the urinary bladder

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4
Q

Pilocarpine

A

Partial muscarinic agonist
-Tertiary amine
-Stable to hydrolysis by acetylcholinesterase
Use: Glaucoma
-Treatment of dry mouth due to radiotherapy for cancer of head and neck

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5
Q

Nicotine

A

Agonist at nicotinic receptors
-Tertiary amine
-Depending on the dose, nicotine depolarizes autonomic ganglia, resulting first in stimulation and then paralysis
-Low doses: ganglionic stimulation by depolarization
-Response resembles simultaneous discharge of both parasympathetic and sympathetic nervous systems
-High doses: ganglionic blockage and neuromuscular blockade
Use: Smoking cessation therapy

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6
Q

Muscarinic Agonists: Adverse effects

A

-Sweating
-Salivation
-Flushing
-Low blood pressure
-Nausea
-Abdominal pain
-Diarrhea
-Bronchospasm

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7
Q

Edrophonium

A

Binds reversibly to the active site of the enzyme
-Inhibition is short-lived

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8
Q

Carbamates

A

Form a covalent bond with the enzyme
-Physostigmine
-Neostigmine
-Pyridostigmine

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9
Q

Organophosphates

A

Phosphorylate the enzyme. The covalent bond formed is extremely stable and hydrolyzes very slowly
-Malathion
-Sarin

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10
Q

Indirect-acting Cholinergic Agents (Anticholinesterases)

A

MOA: cholinesterase inhibitors act by inhibiting acetylcholinesterase: they increase concentration of endogenous acetylcholine

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11
Q

Effects on the Cardiovascular System

A

Vascular smooth muscle: cholinesterase inhibitors have minimal effects because most vascular beds lack cholinergic innervation

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12
Q

Effects on the Neuromuscular Junction

A

Cholinesterase inhibitors increase strength of contraction
-Useful to reverse action of nondepolarizing neuromuscular blockers
-Useful in myasthenia gravis

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13
Q

Edrophonium

A

Quaternary ammonium
-Does not enter CNS
-Diagnosis of myasthenia gravis: this agent leads to rapid increase in muscle strength
-Used to reverse the neuromuscular block produced by non-depolarizing muscular blockers

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14
Q

Physostigmine

A

Tertiary amine
-Can enter and stimulate CNS
-Use: treatment of overdoses of anticholinergic drugs

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15
Q

Neostigmine

A

Quaternary ammonium
-Dose not enter CNS
Use: Urinary retention
-Reversal of effects of non-depolarizing neuromuscular blockers after surgery
-Treatment of myasthenia gravis

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16
Q

Pyridostigmine

A

Quaternary ammonium
-Does not enter CNS
-Treatment for myasthenia gravis

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17
Q

Organophosphates

A

-Synthetic compounds:
Many are extremely toxic
-Insecticides: Malathion (fogging on campus for example)
-Sarin: synthetic toxic agent used in terrorist attack in Japan

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18
Q

Atropine

A

-Prototype of muscarinic antagonists
-Reversible competitive antagonist at muscarinic receptors
-Tertiary amine: both central and peripheral muscarinic blocker

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19
Q

Actions of Atropine

A

M3: blockage:
Eye: Mydriasis & cycloplegia
GI: Reduces gastric motility
Urinary system: Decreases hypermotility of urinary bladder
Secretions: Salivary, sweat and lachrymal glands are blocked
-Inhibition of sweat glands may cause high body temperature

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20
Q

Atrial M2 blockade

A

CV system: Moderate to high therapeutic doses cause tachycardia

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21
Q

Belladonna Alkaloids

A

Uses: Antidote for cholinergic agonists
-Blocks respiratory tract secretions prior to surgery

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22
Q

Adverse effects of belladonna alkaloids

A

Dry mouth
Blurred vision
Sandy eyes
Tachycardia
Constipation
Urinary retention

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23
Q

Belladonna Alkaloids effects on CNS

A

-Restlessness
-Confusion
-Hallucinations
-Delirium

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24
Q

Scopolamine

A

Prevention of motion sickness

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25
Q

Quaternary Ammonium Muscarinic Antagonists

A

Ipratropium

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26
Q

Uses for Ipratropium

A

Treatment of chronic obstructive pulmonary disease (COPD)
-Asthma

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27
Q

Tertiary Amine Muscarinic Antagonists

A

Tropicamide

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28
Q

Uses for Tropicamide

A

Mydriatic for fundoscopy
-Produces mydriasis with cycloplegia

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29
Q

Contraindications of Antimuscarinic Agents

A

-Contraindicated in patients with angle-closure glaucoma
-Should be used with caution in patients with prostatic hypertrophy and in the elderly

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30
Q

Ganglion Blockers

A

Hexamethonium was used for hypertension in the past
-Due to their adverse effects, ganglion blockers have been replaced by superior antihypertensive agents

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31
Q

Pharmacological properties

A

-Effects of ganglion blockers can be predicted by a knowledge of which division of the ANS exercises dominant control of various organs
-The effect of the ganglion blocker is to remove the dominant control

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32
Q

Ganglion blockade may occur by the following mechanisms:

A

1) Prolonged depolarization (Ex. Nicotine)
2) Antagonism of nicotinic receptors (Ex. Hexamethonium)

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33
Q

Two types of neuromuscular blockers

A

1) Tubocurarine (Competitive Antagonists: Non-depolarizing blockers)
2) Succinylcholine (Agonists: Depolarizing Blockers)

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34
Q

Tubocurarine

A

Uses: As adjuvant drugs in anesthesia during surgery to relax skeletal muscle
MOA: Competitive antagonists

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35
Q

Succinylcholine

A

Uses: Rapid endotracheal intubation
-Electroconvulsive therapy (ECT)
MOA: Succinylcholine binds to the nicotinic receptor and depolarizes the junction
-Persists in the synaptic cleft, stimulating the receptor: receptor desensitizes
-This leads to flaccid paralysis

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36
Q

Drugs that act presynaptically: Inhibitors of acetylcholine release

A

-Botulinum Toxin

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37
Q

Uses of Botulinum Toxin

A

Injected locally into muscles for treatment of severe diseases involving muscle spasms
-Approved for cosmetic treatment of facial wrinkles

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38
Q

Adrenergic drugs can treat which kinds of disorders?

A

-Hypertension
-Angina
-Heart Failure
-Arrhythmias
-Asthma
-Migraine
-Anaphylactic reactions

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39
Q

Norepinephrine has [ 1 ] effect on [ 2 ] receptors, therefore it cannot cause bronchodilation, because receptors in bronchial [ 3 ] muscle are [ 4 ].

A

1) Little effect
2) Beta-2
3) Smooth muscle
4) Beta-2

Norepinephrine has little effect on beta-2 receptors, therefore it cannot cause bronchodilation, because receptors in bronchial smooth muscle are beta-2.

40
Q

Epinephrine

A

Potent bronchodilator.

41
Q

Skin blood vessels express almost exclusively what type of receptors?

A

alpha-1 receptors

42
Q

Low concentrations of epinephrine cause: [ ]

A

Vasodilation

43
Q

Locations of Beta-1 receptors

A

1) Heart
2) Juxtaglomerular cells (Kidney)
3) Adipocytes

44
Q

Response of Beta-1 receptors signaling

A

1) increases cAMP, couples with Gs (G-protein coupled receptors)

45
Q

Effects of Beta-1 receptors signaling on the heart

A

1) Increases heart rate
2) Heart force
3) AV conduction velocity

46
Q

Effects of beta-1 receptors signaling on juxtaglomerular cells

A

Increased renin release

47
Q

Effects of beta-1 receptors signaling on adipocytes

A

Increased lipolysis

48
Q

Effects of beta-2 receptor signaling

A

increases cAMP, Couples via Gs

49
Q

Locations of beta-2 receptors

A

1) Smooth Muscle: Relaxation
2) Skeletal muscle: increased glucogenolysis, increased K+ uptake
3) Pancreatic beta-cells: increased insulin secretion
4) Pancreatic alpha-cells: increased glucagon secretion
5) Liver: increased glucogenolysis, increased gluconeogenesis
6) Adipocytes: increased lipolysis

50
Q

Locations of beta-3 receptors

A

Adipocytes

51
Q

Signaling of beta-3 receptors

A

increased cAMP, couples via Gs

52
Q

Locations of alpha-1 receptors

A

1) Vascular smooth muscle
2) Genitourinary smooth muscle
3) Liver

53
Q

Signaling of alpha-1 receptors

A

Increased IP3 and DAG
Increased Ca2+, couples via Gq

54
Q

Effects of alpha-1 receptors on vascular smooth muscle

A

Contraction

55
Q

Effects of alpha-1 receptors on the liver

A

increased glucogenolysis and gluconeogenesis

56
Q

Locations of alpha-2 receptors

A

1) Presynaptic nerve terminals
2) Platelets
3) Adipocytes
4) Pancreatic beta-cells
5) Vascular smooth muscle

57
Q

Signaling action of alpha-2 receptors

A

Decreased cAMP
Couples via Gs

58
Q

Effects of alpha-2 receptors on presynaptic nerve terminals

A

Inhibition of NE release

59
Q

Effects of alpha-2 receptors on platelets

A

Aggregation

60
Q

Effects of alpha-2 receptors on adipocytes

A

Inhibition of lipolysis

61
Q

Effects of alpha-2 receptors on pancreatic beta-cells

A

decreased insulin secretion

62
Q

Effects of alpha-2 receptors on vascular smooth muscle

A

Contraction

63
Q

D1, D5 receptor locations

A

Smooth muscle of the renal vascular bed

64
Q

D1,D5 signaling action

A

increases cAMP

65
Q

D1, D5 effects on smooth muscle of the renal vascular bed

A

relaxation

66
Q

Epinephrine action

A

Acts as a hormone, after release from the adrenal medulla into the blood it acts on distant cells.
-Agonist at both alpha and beta adrenoceptors

67
Q

At low concentrations, epinephrine activates mainly [ ] receptors

A

beta-1 and beta-2

68
Q

At higher concentrations, [ ] effects become more pronounced

A

alpha-1 effects

69
Q

Isoproterenol

A

-May be used in emergencies to stimulate heart rate in patients with bradycardia or heart block
-Increases heart rate, force of contraction and cardiac output
-Dilates arterioles of skeletal muscle, resulting in a decrease in peripheral vascular resistance

70
Q

Dobutamine

A

-Predominantly a beta-1 agonist.
-Given IV
-Potent inotrope, with comparatively mild chronotropic effects.
-Produces less increase in HR and less decrease in PVR than isoproterenol
-Increases myocardial O2 consumption
-Basis of the dobutamine stress echocardiogram

71
Q

Albuterol

A

Causes bronchodilation
-Used in asthma
-DOC for acute asthma attacks

72
Q

Phenylephrine

A

Causes vasoconstriction alpha-1 effect
Used for: Nasal decongestant (orally or topically)
-Mydriatic (dilation of pupils)

73
Q

Clonidine

A

Partial alpha-2 agonist
-Centrally acting antihypertensive
-Reduces sympathetic outflow, reduces BP

74
Q

Releasing agents

A

Amphetamine
Tyramine

75
Q

Uses for amphetamine

A

Central stimulatory action
-Can increase BP by alpha-agonist action on vasculature as well as beta-stimulatory effects on the heart
Used for treatment of: ADHD, Narcolepsy

76
Q

Tyramine

A

Found in fermented foods such as ripe cheese and Chianti wine
-MAO inhibitors (antidepressants)

77
Q

Cocaine

A

Blocks monoamine reuptake
-Monoamines accumulate in synaptic space

78
Q

Mixed acting adrenergic agonists

A

Ephedrine
Pseudoephedrine

79
Q

Ephedrine

A

Penetrates the CNS
Used as: pressor agent, particularly during spinal anesthesia

80
Q

Pseudoephedrine

A

One of 4 ephedrine enantiomers
-Sudafed over the counter component of many decongestant mixtures

81
Q

Non-selective alpha-adrenergic blockers

A

Phenoxybenzamine
Phentolamine

82
Q

Alpha-1 selective adrenergic blockers

A

Prazosin
Terazosin
Doxazosin
Tamsulosin

83
Q

Phenoxybenzamine

A

Irreversible antagonist
Used to treat: Pheochromocytoma (pre-op surgical removal of a tumor)
-Chronic management of inoperable tumors

84
Q

Phentolamine

A

Used to diagnose pheochromocytoma: control of hypertension during preoperative preparation and surgical excision
-Phentolamine blocking test
-Prevention of dermal necrosis after extravasation of norepinephrine
-Cocaine-induced acute coronary syndrome: to reverse coronary artery vasoconstriction

85
Q

Treatment of hypertension and BPH

A

Terazosin
Doxazosin

86
Q

Tamsulosin

A

Selective for alpha-1A receptors
-Approved for BPH
-Little effect on BP
-Less likely to cause orthostatic hypotension

87
Q

Which kinds of drugs are contraindicated in patients with asthma?

A

beta-blockers

88
Q

Non-selective beta-blockers

A

Propranolol
Nadolol
Timolol

89
Q

Metabolic effects of beta blockers

A

1) Decreased glycogenolysis
2) Decreased glucagon secretion

90
Q

Atenolol

A

Useful in hypertensive patients with impaired pulmonary function

91
Q

Metoprolol

A

Useful in diabetic hypertensive patients who are receiving insulin or oral hypoglycemic agents

92
Q

Esmolol

A

Ultra-short acting
-IV administration
-Used for rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter

93
Q

Pindolol

A

May be preferred in individuals with diminished cardiac reserve or a propensity to bradycardia

94
Q

Labetalol

A

Competitive antagonist at beta and alpha-1 receptors
-Substantially more potent as a beta-antagonist than as an alpha-antagonist
-Used in hypertension

95
Q

Carvedilol

A

Similar to labetalol
-Antioxidant properties
-Used in hypertension and CHF

96
Q

Adverse effects of beta-blockers

A

1) Bronchoconstriction
2) Hypoglycemia
3) Lipid metabolism
CNS effects: Sedation, Dizziness, Lethargy, Fatigue

Term 1 MD (54 decks)

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