High Yield – Pharmacology USMLE

a1 receptor (class q)
Vascular smooth muscle contraction, ↑pupillary dilation (mydriasis), intestinal and bladder sphincter contraction, ↓Renin, NO CYCLOPLEGIA, can cause sexual disfunction, ↑TPR, and ↑After-load

a2 receptor (class i)
↓sympathetic release ↓insulin release ↓lipolysis ↑platelet aggregation(epinephrine). ↓cAMP

b1 receptor (class s)
↑heart rate and contractility, ↑renin release, ↑cAMP, ↑lipolysis (+inotropic)

b2 receptor (class s)
vasodilation, bronchodilation, ↓uterine tone (tocolysis), DOES NOT USE NE. All blood vessels affected. ↑HR, ↑contractility, ↑lipolysis, ↑insulin release, ciliary muscle relaxation, ↑aqueous humor production, ↑gluconeogenesis

M1 receptor (class q)
CNS, gastric parietal cells (↑H+ production). Contraindicated for PUD.

M2 receptor (class i)
decreased heart rate and atrial contractility

M3 receptor (class q)
stimulates glandular secretions (lacrimal,sweat, gastric), ↑gut peristalsis, ↑pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation), ↑bladder contraction. Contraindicated for COPD/Asthma patients.

D1(Dopamine) receptor (class s)
renal vascular smooth muscle relaxation via vasodilation. Typical drug “Fenoldopam” which ↑RBF, ↑GFR, ↑Na+ secretion

D2 receptor (class i)
↓sympathetic release, modulates transmitter release (especially in brain)

H1(Histamine) receptor (class q)
↑sinus and bronchial mucus production, ↑vascular permeability, bronchial constriction, itching(pruritus), and pain

H2 receptor (class s)
increased gastric acid secretion

V1(Vasopressin) (class q)
vascular smooth muscle contraction

V2 (class s)
↑H2O reabsorption in collecting tubules of kidneys. Found in kidneys

Muscarinic and Nicotinic receptors are located where?
They are located on the post-synaptic terminal located on the effector cells

The re-uptake of Choline into the pre-synaptic terminal is inhibited by what?
Hemicholinium

Vesamicol inhibits what process?
uptake of ACh into the synaptic vesiclec causing a release in the reduction of ACh.

Botulinum Toxin inhibits what process?
release of ACh from the vesicles

What receptor does the somatic motor neuron synapse with?
Neuromuscular junction using ACh with (Nm receptor) on skeletal muscle

Metyrosine inhibits what process?
Conversion of Tyrosine Hydroxylase to Dopa

what is MAO-A
MAO-A is the metabolic process for the Adrenergic nerve terminal. It also takes part in supplying the NE mobile pool and is converted into VMA in the urine. COMT is methylated and oxidized by MAO

Name 3 drugs that inhibit the reuptake of NE and are indirect general agonist (sympathomimetics)
Cocaine, TCA’s, and Amphetamines

Out of the 3 drugs that inhibit the reuptake of NE, which drug’s also releases stored catecholamines?
Amphetamine and Ephedrine

Where is Phenylalanine made?
The liver

Which drugs inhibit the the release of stored catecholamines?
Bretylium and guanethidine

AChE inhibitors act on what process?
AChE inhibitors prevent the uptake of AChE on the post-synaptic membrane

Reserpine’s effect on the Noradrenergic membrane is?
inhibits the uptake of dopamine into the storing vesicle

What is the process of Guanethidine?
Guanethidine prevents the release of (exocytosis) of NE

What are the Direct Cholinomimetic muscarinic agonist (paraysympathomimetics) drugs?
Bethanechol, Carbachol, Pilocarpine, and Methacholine

Bethanechol
Muscarinic agonist. Longer acting than ACh (resistant to AChE). Treatment of ileum and urinary retention. Bowels and Bladder!

Carbachol
Muscarinic/nicotinic agonist. Applied to eye to causes contraction of ciliary muscle, relief of open-angle glaucoma. Also constricts pupil

Pilocarpine
Muscarinic agonist. Stimulates tears, sweat, and Saliva. Constricts pupil and ciliary muscle. Also used for acute glaucoma

Methacholine
Muscarinic Agonist. Causes bronchoconstruction when inhaled. Used for asthma challenge test.

What are the 6 Anticholinesterases (indirect cholinomimetics?)
Neostigmine, Pyridostigmine, Edriphonuim, Physostigmine, Echothiophate, and Donepezil

Neostigmine
Quaternary amine. Treatment of of ileum, urinary retention, and MG. Post-op reversal of neuromuscular junction blockade (Nm)

Pydriostigmine
Quaternary amine. Treatment of MG. Long acting

Edrophonium
Very short acting (10-20 mins.) Diagnosis of MG via anti-AChR Ab test.

Physostigmine
Tertiary amide (can enter CNS). Treatment of glaucoma. Antidote for atropine toxicity

Donepezil
Alzheimer disease. Increase of endogenous ACh

What are the negative effects of cholinomimetic agents?
exacerbation of COPD, asthma, and peptic ulcers

What are the cholinesterase inhibitor poisoning symptoms?
DUMBBELSS (Diarrhea, Urination, Miosis, Bronchoconstriction, Bradycardia, Excitation (skeletal muscle and CNS), Lacrimation, Salivation

What is the treatment for cholinesterase inhibitor poisoning?
Atropine (Muscarinic Antagonist), and Pralidoxime (2PAM) which regenerates Cholinesterase.

What are some muscarinic receptor anatagonist (anti-muscarinic)
Atropine, Antihistamines, tricyclic antidepressants, Antipsychotics, Quinidine, Amantadine, Meperidine, Ipratropium, Scopolamine, Benztropine, trihexyphenidyl, Tropicamide

How does a muscarinic receptor antagonist work?
Tertiary amine. Opposite effects of DUMBBELSS. decreased epithelial secretions, mydriasis, cycloplegia, hyperthermia, vasodilation, tachycardia, sedation, urinary retention, constipation

Atropine
antispasmodic, antisecretory, management of AChE inhibitor OD, antidiarrheal, ophthalmology (long acting)

Tropicamide
Ophthalmology (topical)

Ipratropium
Asthma and COPD (no change in mucus viscosity)

Scopolamine
treats motion sickness and causes sedation and short term memory block

Beztropine/Trihexyphenidyl
Lipid-soluble. Used in parkinsonism and in acute extrapyramidal symptoms induced by antipsychotics

Hexamethonium (nicotinic antagonist)
Used to prevent vagal reflexes due to sympathetic stimulation. Can be used to prevent reflex bradycardia caused by increased bp due to increased norepinephrine. Excess hexamethonium can cause orthostatic hypotension, blurred vision, constipation.

Name 11 Direct Sympathomimetics
Epinephrine, Norepinephrine, Isoproterenol, Dopamine, Dobutamine, Ritodrine, Metaproterenol, Albuterol, Salmeterol, Terbutaline, and Phenylephrine

Epinephrine
Function: a, B agonist. Clinical Usage: Treatment of anaphylaxis, open-angle glaucoma, asthma, hypotension. Prolongs the effect of local anesthesia. Adverse effects: Increased systolic blood pressure + decreased blood pressure=widened pulse pressure

Norepinephine
Function: Mainly a-receptor agonist, but has some B-receptor activity. Clinical usage: Treatment of hypotension. Adverse effects: Splanchnic vasoconstriction and decreased renal perfusion, increased systolic, increased diastolic=little/no change in pulse pressure. Reflexive decrease in heart rate

Isproterenol
B1B2 agonist. Treatment of AV conduction block. Decrease in diastolic BP (induces reflexive increase in heart rate)

Dopamine
D1=D2>B> a agonist. Inotropic and chronotropic. Treatment for shock, especially with heart failure

Dobutamine
B1>B2 agonist. Inotropic. Treatment of heart failure. Used in cardiac stress test

Ritodrine
B2 agonist. Reduces premature uterine contractions

metaproterenol & albuterol
selective B2 agonists (B2>B1). Treatment of asthma (acute)

Salmeterol
selective B2 agonist (B2>B1). Long-acting treatment of asthma

Terbutaline
selective B2 agonist (B2>B1). Treatment of asthma

Name 4 indirect sympathomimetics
Amphetamine, Ephedrine, Cocaine, Tyramine,

Amphetamine
Indirect general agonist (sympathomimetic). Re-uptake inhibitor. Induces catecholamine release from terminals. Treatment for narcolepsy, obesity, and ADHD. a1 agonist which increases BP

Ephedrine
Indirect general agonist. Induces catecholamine release. Treatment for nasal congestion, urinary incontinence, hypotension (HTN crisis). Penetrates CNS

Cocaine
Indirect general agonist. Inhibits reuptake of catecholamines. Vasoconstriction, local anesthetic. Never give B-Blockers if cocaine intoxication is suspected. Can lead to a1 activation causing extreme hypertension.

Tyramine
Similar mechanism to amphetamines, cleared by MAO (MAO inhibitors can cause hypertension, especially with tyramine-rich foods such as wine and cheese).

Name 2 sympathoplegics
a-methyldopa and clonidine

Clonidine
Agonist of central a2-adrenergic receptors which decreases sympathetic outflow

a-methyldopa
used to treat hypertension by decreasing sympathetic tone

What are the non-selective (a1 and a2) Alpha-blockers?
Phenoxybenzamine and phentolamine

What are phenoxybenzamine and phentolamine used for?
Treatment of pheochromocytoma. Also used to treat Raynaud’s syndrome

What are the a1-selective Alpha blockers? (ZOSIN)
Prazosin, Terazosin, and Doxazosin

Prazosin
Treatment of HTN, urinary retention (BPH).

Terazosin
Treatment of HTN, urinary retention (BPH). May cause orthostatic hypotension

Doxazosin
Treatment of HTN, urinary retention (BPH). Usually taken at bedtime

Name the a2-selective Alpha blocker
Mirtazapine

Mirtazapine
Treatment of depression. Can cause sedation, increased serum cholesterol, and increased appetite

What are the non-selective (b1 and b2) Beta blockers? (olol)
Propranolol (migranes), Timolol (glaucoma), Nadolol

What are the b1 selective Beta blockers
Metoprolol, Atenolol, Betaxolol, Esmolol (very short acting)

What are the mixed a and b blockers Beta blockers?
Carvedilol and Labetalol

What are the partial b-agonist
Pindolol and acebutolol

Propranolol
Beta 2 receptor blocker: used for sedation, thyrotoxicosis, performance anxiety, and essential tremor. Inquired in plasma lipids

Timolol
B2 receptor antagonist. Used to treat Glaucoma.

Nadolol
Beta2 blocker. Treats HTN and Angina

Pindolol
B2 blocker

Metoprolol
Beta 1 blocker. Used to treat HTN and Angina for survival of heart attack. (extended release) Long acting.

Atenolol
Beta 1 blocker. Used to treat HTN and prevent Angina.

Betaxolol
Beta 1 blocker. Used to treat open angle glaucoma, HTN, and Angina

Esmolol
Beta 1 blocker. Used to treat A. Fib and arrhythmia.

Carvedilol
Beta blocker. Used to treat severe heart failure

Labetalol
Beta blocker. Used to treat HTN. Used for chronic treatment of high blood pressure during pregnancy.

Pindolol
partial beta-receptor (agonist) drug used as a local anesthetic. Moderate lipid solubility. Elimination half-life 3-4 hrs. Also used for HTN and angina.

Acebutolol
Beta blocker. Used to treat HTN and irregular heart rate (arrhythmia)

Beta blockers that start with A-M
are B1 blockers

Beta blockers that start with N-Z
are B2 blockers

Beta-blocker treatment for HTN
decreased CO, decreased renin production (b1-blockade of JG cells). JG cells release Renin

Beta-blocker treatment for Angina
decreased HR, decreased isotropy, decreased myocardial O2 consumption

Beta-blocker treatment for MI
decreased mortality with use of metoprolol, carvedilol, and bisoprolol

Beta-blocker treatment for SVT
propanolol/esmolol to decrease AV conduction.

Heart failure (CHF)
slows progression of CHF (decreased cardiac demand)

Side effects of Beta-blockers include?
Exacerbation of asthma, impotence, bradycardia, AV blockade, sedation, Decreased glucagon secretion

Propranolol *Nonselective *Low dose-dependent bioavailability Negligible effects on alpha and muscarinic receptors *Nitric Oxide partial agonist activity at beta-receptors Metoprolol *Beta-1 selective (preferable in pts. with diabetes or PVD) Better for pts. who experience bronchoconstriction w/ propranolol but still use …

alpha 1- found where? – vascular smooth muscle in skin and gut alpha 1- effect? – activates vasoconstriction – during flight or fight want reduced blood flow to skin and gut – End result: VASOCONSTRICTION at skin and gut WE …

What components of the sympathetic nervous system are innervated by cholinergic fibers? adrenal medulla and sweat glands ACh acts are 2 types of receptors: nicotinic and muscarinic. What types of receptors are these? nicotinic ACh receptors are Na+/K+ channels muscarinic …

Chronic inflammatory reversible disease of tracheobronchial airways characterized by airflow obstruction and increased responsiveness to a variety of stimuli asthma – inflammation of bronchial wall – increased mucus secretion – bronchiolar smooth muscle constriction List 3 s/s of bronchoconstriction. chest …

First-Pass Effect Drug absorbed from GI tract and carried to the liver through portal circulation. Some drugs extensively metablized by liver. Only part of drug reaches systemic circulation for distribution theses types of drugs should not be administered PO (lidocaine/some …

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