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USMLE Step 1. > Intro Pharm > Flashcards

Intro Pharm Flashcards

1
Q

Alpha1 receptors

A

Sympathetic

Linked with Gq proteins

1) Increase vascular smooth muscle contraction
2) Increase pupillary dilator muscle contraction (mydriasis)
3) Increase intestinal and bladder sphincter muscle contraction

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2
Q

Alpha2 receptors

A

Sympathetic

Linked with Gi proteins

1) Lower sympathetic outflow
2) Lower insulin release
3) Lower lipolysis
4) Increase platelet aggregation
5) Lower aqueous humor production

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3
Q

B1 receptors

A

Sympathetic

Linked with Gs proteins

1) Increase HR
2) Increase Contractility
3) Increase renin release
4) Increase Lipolysis

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4
Q

B2 receptors

A

Sympathetic

Linked with Gs proteins

1) Vasodilation
2) Bronchodilation
3) Increase lipolysis
4) Increase insulin release
5) Lower uterine tone (tocolysis)
6) Ciliary muscle relaxation
7) Increase aqueous humor production

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5
Q

M1 receptors

A

Parasympathetic

Linked with Gq proteins

1) CNS
2) Enteric Nervous System

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6
Q

M2 receptors

A

Parasympathetic

Linked with Gi proteins

1) Lower HR
2) Lower contractility of atria

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7
Q

M3 receptors

A

Parasympathetic

Linked with Gq proteins

1) Increase exocrine gland secretions (lacrimal, salivary, gastric acid)
2) Increase gut peristalsis
3) Increase bladder contraction
4) Increase bronchoconstriction
5) Increase pupillary sphincter muscle contraction (miosis)
6) Increase ciliary muscle contraction (accommodation)

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8
Q

D1 receptor

A

Dopamine

Linked with Gs proteins

Relaxes renal vascular smooth muscle

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9
Q

D2 receptor

A

Dopamine

Linked with Gi proteins

Modulates transmitter release, esp in brain

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10
Q

H1 receptor

A

Histamine

Linked with Gq proteins

1) Increased nasal and bronchial mucus production
2) Increased vascular permeability, contraction of bronchioles, pruritis, and pain

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11
Q

H2 receptor

A

Histamine

Linked with Gs proteins

Increases gastric acid secretion

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12
Q

V1 receptor

A

Vasopressin

Linked with Gq proteins

Increase vascular smooth muscle contraction

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13
Q

V2 receptor

A

Vasopressin

Linked with Gs proteins

Increase H2O permeability and reabsorption in collecting tubules of kidney.

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14
Q

Bethanechol

A

Cholinomimetic Direct Muscarinic Agonist

Use: Postoperative ileus, neurogenic ileus, urinary retention

Activates bowel and bladder smooth muscle; resistant to AChE

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15
Q

Carbachol

A

Cholinomimetic - Direct Muscarinic agonist

Use: Constricts pupil and relieves intraocular pressure in glaucoma

Carbon copy of acetylcholine

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16
Q

Methacholine

A

Cholinomimetic - Direct Muscarinic agonist

Use: Challenge test for diagnosis of asthma

Stimulates muscarinic receptors in airway when inhaled

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17
Q

Pilocarpine

A

Cholinomimetic - Direct Muscarinic agonist

Use: Potent stimulator of sweat, tears, and saliva. Open angle and close-angle glaucoma

Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma); resistant to AChE

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18
Q

Donepezil
Galantamine
Rivastigmine

A

Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase

Use: Alzheimer

Increase ACh

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19
Q

Edrophonium

A

Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase

Use: Historically, diagnosis of myasthenia gravis (extremely short acting). Myasthenia now diagnosed by anti-AChR Ab (anti-acetylcholine receptor antibody) test.

Increases ACh

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20
Q

Neostigmine

A

Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase

Use: Postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postop)

Increases ACh

No CNS penetration

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21
Q

Physostigmine

A

Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase

Use: Anticholinergic toxicity; crosses BBB into CNS

Increases ACh

For Atropine overdose

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22
Q

Pyridostigmine

A

Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase

Use: Myasthenia gravis (long acting); does not penetrate CNS

Increases ACh

Increases muscle strength

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23
Q

Cholinomimetic (Muscarinic agonist) cautions

A

For all of these agents, look out for exacerbation of COPD, asthma, and peptic ulcers when giving to susceptible patients.

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24
Q

Cholinesterase inhibitor poisoning

A

Often due to organophosphates such as parathion that irreversibly inhibit AChE.

Diarrhea
Urination
Miosis
Bronchospasm 
Bradycardia
Excitation of skeletal muscle and CNS
Lacrimation
Sweating
Salivation

DUMBBELSS

Organophosphates are often components of insecticides; poisoning usually seen in farmers.

Antidote = atropine (competitive inhibitor) + pralidoxime (regenerates AChE if given early)

25
Atropine Homatropine Tropicamide
Muscarinic antagonists/anticholinergics Act at Eye Use: Produces mydriasis and cycloplegia
26
Benztropine
Muscarinic antagonists/anticholinergics Act in CNS Uses: Parkinson Disease Acute dystonia
27
Glycopyrrolate
Muscarinic antagonists/anticholinergics Acts in GI, respiratory Uses: Parenteral - preop use to reduce airway secretions Oral - drooling, peptic ulcer
28
Hyoscyamine | Dicyclomine
Muscarinic antagonists/anticholinergics GI Uses: Antispasmodic for IBS
29
Ipratropium | Tiotropium
Muscarinic antagonists/anticholinergics Respiratory Use: COPD Asthma
30
Oxybutynin Solifenacin Tolterodine
Muscarinic antagonists/anticholinergics GU Use: Reduce bladder spasms and urge urinary incontinence (overactive bladder)
31
Scopolamine
Muscarinic antagonists/anticholinergics CNS Use for motion sickness
32
Atropine
Muscarinic antagonist/anticholinergic Used to treat bradycardia and for ophthalmic applications ``` Eye: Increases pupil dilation, cycloplegia Airway: Lowers secretions Stomach: Lower acid secretion Gut: Lower motility Bladder: Lower urgency in cystitis ``` Toxicity: Increased body temp (due to less sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation Can cause acute-angle closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia and hyperthermia in infants ``` Hot as a hare Dry as a bone Red as a beet Blind as a bat Mad as a hatter ``` Jimson weed (datura) leads to gardener's pupil (mydriasis due to plant alkaloids)
33
Tetrodotoxin
Highly potent toxin that binds fast voltage-gated Na channels in cardiac and nerve tissue, preventing depolarization (blocks action potential without changing resting potentials). Causes nausea, diarrhea, paresthesias, weakness, dizziness, loss of reflexes Tx is primarily supportive Poisoning can come from ingestion of poorly prepared pufferfish (fugu), a Japanese delicacy
34
Ciguatoxin
Causes ciguatera fish poisoning. Opens Na channels causing depolarization Symptoms easily confused with cholinergic poisoning Temperature-related dysesthesia (cold feels hot; hot feels cold) is regarded as a specific finding of ciguatera Tx is supportive Comes from eating reef fish - barracuda, snapper, moray eel
35
Scombroid poisoning
Acute-onset burning sensation of the mouth, flushing of face, erythema, urticaria, pruritis, headache. May cause anaphylaxis-like presentation (bronchospasm, angioedema, hypotension) Tx supportively with antihistamines; if needed, antianaphylactics (bronchodilators, Epi) Caused by consumption of dark-meat fish (bonito, mackerel, mahi-mahi, tuna) improperly stored at warm temps. Bacterial histidine decarboxylase converts histidine to histamine. Histamine is not degraded by cooking. Frequently misdiagnosed as allergy to fish
36
Albuterol | Salmeterol
Sympathomimetics - Direct B2 > B1 Albuterol for acute asthma Salmeterol for long term asthma or COPD control
37
Dobutamine
Sympathomimetic - Direct B1 > B2, Alpha ``` Heart failure (inotropic > chronotropic) Cardiac stress testing ```
38
Dopamine
Sympathomimetic - Direct D1 = D2 > B > alpha Unstable bradycardia HF Shock Inotropic and chronotropic alpha effects predominate at high doses
39
Epinephrine
Sympathomimetic - Direct B > alpha Anaphylaxis Asthma Open-angle glaucoma Alpha effects predominate at high doses Significantly stronger effect at B2 receptor than NE
40
Isoproterenol
Sympathomimetic - Direct B1 = B2 Electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia
41
Norepinephrine
Sympathomimetic - Direct Alpha1 > alpha2 > B1 Hypotension (but lowers renal perfusion) Significantly weaker effect at B2-receptor than Epi
42
Phenylephrine
Sympathomimetic - Direct Alpha1 > alpha2 ``` Hypotension (vasoconstrictor) Ocular procedures (mydriatic) Rhinitis (decongestant) ```
43
Amphetamine
Sympathomimetic - Indirect Indirect general agonist, reuptake inhibiter, also releases stored catecholamines For: Narcolepsy, obesity, ADHD
44
Cocaine
Sympathomimetic - Indirect Indirect general agonist, reuptake inhibiter Causes vasoconstriction and local anesthesia. Never give B-blockers if cocaine intoxication is suspected (can lead to unopposed alpha 1 activation and extreme hypertension)
45
Ephedrine
sympathomimetic - Indirect Indirect general agonist, releases stored catecholamines Nasal decongestion, urinary incontinence, hypotension
46
Clonidine
Alpha 2 agonist For: hypertensive urgency (limited situations); does not decrease renal blood flow ADHD Tourette Syndrome Toxicity: CNS depression, bradycardia, hypotension, respiratory depression, miosis
47
Alpha-methyldopa
Alpha 2 agonist For: HTN during pregnancy Toxicity: Direct Coombs (+) hemolysis SLE-like syndrome
48
Nonselective alpha blockers
Phenoxybenzamine (irreversible) | Phentolamine (reversible)
49
Phenoxybenzamine
Nonselective alpha blocker (irreversible) Uses: Pheochromocytoma (used preop) to prevent catecholamine (hypertensive) crisis Side effects: Orthostatic hypotension, reflex tachycardia
50
Phentolamine
Nonselective alpha blocker (reversible) Uses: Give to patients on MAOIs who eat tyramine-containing foods Side effects: Orthostatic hypotension, reflex tachycardia
51
Alpha 1 selective alpha blockers
Prazosin Terazosin Doxazosin Tamsulosin
52
Prazosin Terazosin Doxazosin Tamsulosin
Alpha 1 selective alpha blockers Uses: Urinary symptoms of BPH; PTSD (prazosin); HTN (not tamsulosin) Side effects: 1st dose orthostatic hypotension, dizziness, HA
53
Alpha 2 selective alpha blockers
Mirtazapine
54
Mirtazapine
Alpha 2 selective alpha blocker Uses: Depression Side effects: Sedation, high serum cholesterol, high appetite
55
B1 selective antagonists
B1 > B2 ``` Acebutolol (partial agonist) Atenolol Betaxolol Esmolol Metoprolol ```
56
Nonselective Beta antagonists
B1 = B2 Nadolol Pindolol (partial agonist) Propranolol Timolol
57
Nonselective Beta and Alpha antagonists
Carvedilol | Labetalol
58
Nebivolol
Combines cardiac-selective B1-adrenergic blockade with stimulation of B3 receptors, which activate NO synthase in the vasculature
59
Beta Blockers
Uses: 1) Angina pectoris - lower HR and contractility, resulting in lower O2 consumption 2) MI - B-blockers (metoprolol, carvedilol, bisoprolol) lower mortality 3) SVT (metoprolol, esmolol) - lower AV conduction velocity (class 2 antiarrhythmics) 4) HTN - lower Cardiac Output, lower renin secretion (due to B1 receptor blockade on JGA cells) 5) HF - lower mortality in chronic HF 6) Glaucoma (timolol) - lower secretion of aqueous humor Toxicity: Impotence CV adverse effects (bradycardia, AV Block, HF) CNS adverse effects (seizures, sedation, sleep alterations) Dyslipidemia (metoprolol) Asthma/COPD exacerbations Avoid in cocaine users due to risk of unopposed alpha-adrenergic receptor agonist activity Despite theoretical concern of masking hypoglycemia in diabetics, benefits likely outweigh risks; not contraindicated

USMLE Step 1. (19 decks)

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