Reverse pharmacology Flashcards by Tim Horrocks

Direct cholinnomimetic agonist

Postoperative ileus, neurogenic ileus, urinary retention

Activates bladder and bowel smooth muscle

bethanacol

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Direct cholinomimetic agonist

Constricts pupil and relieves intraocular pressure in glaucoma

carbachol

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Direct cholinomimetic agonist

challenge test for diagnosis of asthma

methacholine

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Direct cholinomimetic agonist

Potent stimulator of seat, tears, and saliva
Open angle and closed angle glaucoma

Constracts ciliary muscle of eye (open angle glaucoma)
and pupilary sphincter (closed angle glaucoma)

pilocarpine

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Anticholinesterases (3)

Alzheimers

donezipil, galantamine, and rivastigmine

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Anti AChE

Historically, diagnosis of myasthenia gravis (extremely short acting)

edrophonium

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Anti AChE

Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockage

No CNS penetration

neostigmine

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Anti AChE

Anticholinergic (atropine) toxicity; crosses blood rain barrier

physostigmine

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Anti AChE

Myasthenia gravis (long acting)

No CNS penetration

pyridostigmine

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Muscarinic antagonists (3)

Mydriasis and cycloplegia

atropine
homatropine
tropicamide

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Muscarinic antagonists

Parkinsons
Acute dystonia

Benztropine

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Muscarinic antagonists

Parenteral: Pre op use to reduce airway secretions
Oral: Drooling, peptic ulcer

glycopyrrolate

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Muscarinic antagonists (2)

Antispasmodics for irritable bowel syndrome

hyoscyamine

dicyclomine

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Muscarinic antagonists (2)

COPD, asthma

ipratropium, tiotropium

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Muscarinic antagonists (3)

Reduce bladder spasms and urge incontinence

oxybutynin, solifenacin, tolterodine

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Muscarinic antagonists

Motion sickness (CNS)

scopolamine

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Musc. antag

Incr. pupil dilation/cycloplegia
Decr. airway secretions
Decr. acid secretion in stomach
Decr. motility in gut
Decr. urgency in cystitis

Treats bradycardia
Opthalmic applications
Blocks DUMBBLSS (not CNS or skel. muscle=nicotinic)

Toxicity:

Incr. body temp (decr. sweating)
rapid pulse
dry mouth
dry, flushed skin
cycloplegia
constipation
disorientation

HOT as a hare
DRY as a bone
RED as a beet
BLIND  as a bat
MAD as a hatter

Acute angle closure glaucoma in elderly (mydriasis)
urinary retention in men with prostatic hyperplasia
hyperthermia in infants

Jimson Weed leads to gardner’s pupil (mydriasis due to plant alkaloids)

Atropine

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Dark meat fish improperly stored at warm temp.

Bacterial histidine decarboxyl. converts histadine to histamine which isn’t degraded by cooking.

Misdiagnosed as allergy to fish

Acute onset burning sensation of the mouth, flushing of face, erythema, urticaria, pruritus, headache
Anaphylaxis like presenation is possible

Antihistamines
Possible antianaphylactics

Scombroid

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Reef fish

Opens Na channels causing depolarization

Similar to cholinergic poisoning

Temperature related dysthesias are a specific finding

Supportive

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Ciguatoxin

Very potent: binds fast voltage gated Na channels and prevents depolarization

Pufferfish

Nausea, diarrhea, paresthesias, weakness, dizziness, loss of reflexes

Supportive

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tetrodotoxin

Direct sympathomimetics

beta 2 > beta 1

Acute asthma

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albuterol

Direct sympathomimetics

beta 1 > beta 2
alpha

Heart failure (inotropic > chronotropic)
Cardiac stress testing

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dobutamine

Direct sympathomimetics

D1=D2 > beta > alpha

unstable bradycardia
HF
Shock
Inotropic and chronotropic alpha effects predominate at high doses.

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dopamine

Direct sympathomimetics

Beta > alpha

Anaphylaxis
asthma
open angle glaucoma
Alpha effects predominate at high doses

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epinephrine

Direct sympathomimetics Beta 1 = beta 2 electrophysiologic eval. of tachyarrythmias Can worsen ischemia

isoproterenol

Direct sympathomimetics alpha 1 > alpha 2 > beta 1 hypotension (but decr. renal perfusion)

Direct sympathomimetics alpha 1 > alpha 2 ``` hypotensin (vasoconstrictor) ocular procedures (mydriatic) rhinitis (decongestant) ```

Phenylephrine

Direct sympathomimetic Beta 2 > beta 1 Long term asthma or COPD control

salmeterol

Indirect sympathomimetic Indirect general agonist Reuptake inhibitor Releases stored catecholamines Narcolepsy Obesity ADHD

amphetamine

Indirect sympathomimetic Indirect general agonist reuptake inhibitor Vasoconstriction and local anesthesia Never give beta blocker in intoxication b/c it can lead to unopposed alpha 1 activation and extreme hypertension

Cocaine

Indirect sympathomimetic Indirect general agonist Releases stored catecholamines Nasal congestion Urinary incontinence Hypotension

Ephedrine

sympatholytic (alpha 2 agonist) Hypertensive urgency; does not decr. renal blood flow ADHD Tourette Syndrome CNS Depression bradycardia hypotension resp. depression

clonidine

sympatholytic (alpha 2 agonist) Hypertension in pregnancy Direct coombs + hemolysis SLE like syndrome

alpha methyl dopa

Non selective alpha blocker pheochromocytoma (operatively) to prevent catecholamine crisis

phenoxybenzamine

non select alpha blocker Give to pts. on MAOIs who eat tyramine containing food orthostatic hypertension Reflex tachycardia

\phentolamine\

Alpha 1 selective blockers (2) urinary symptoms of BPH Hypertension 1st dose orthostatic hypotension dizziness headache

terazosin, doxazosin

Alpha 2 selective alpha blocker Depression Sedation Incr. serum cholesterol Incr. appetite

mirtazapine

Alpha 1 selective blockers urinary symptoms of BPH PTSD Hypertension 1st dose orthostatic hypotension dizziness headache

prazosin

Alpha 1 selective blockers urinary symptoms of BPH 1st dose orthostatic hypotension dizziness headache

tamsulosin

Angina: decr. HR and contractility leading to decr. O2 consumption MI: Decr. mortality (3?) SVT: Decr. AV conduction velocity (2?) Hypertension: Decr. CO, Decr. renin secretion HF: Decr. mortality Glaucoma: Decr. secretion of aqu. humor (1?)

Beta blockers (metoprolol, carvedilol, bisoprolol) (class II antiarryth) Metoprolol, esmolol timolol

Beta 1 selective antagonists

acebutolol, atenolol, betaxolol, esmolol, and metoprolol?

Non selective beta antagonists

nadolol, pindolol, propranolol, and timolol?

Partial beta agonists

pindolol and acebutolol

non selective alpha and beta antagonists

carvedilol and labetalol

cardiac selective beta 1 blockade | stimulation of beta 3 leading to NO synthase in vasculature

nebivolol

Toxins fixed by these antidotes? ``` N-acetylcysteine (replenishes glutathione) Atropine > pralidoxime NH4Cl (acidify urine) Physostigmine salicylate, control hyperthermia Flumazenil glucagon 100% O2, hyperbaric O2 penicillamine nitrate + thiosulfate, hydroxocobalamin Anti dig Fab fragments Protamine sulfate Deferoxamine, deferasirox EDTA, dimercaprol, succimer, penicillamine Dimeraprol (BAL), succimer Fomepizole > ethanol, dialysis methylene blue, vitamin C naloxone, naltrexone NAHCo3 (alkalinize urine), dialysis NaHCO3 (plasma alkalinize) Aminocaproic acid Vitamin K (delayed) FFP (immediate) ```

acetaminophen: N-acetylcysteine (replenishes glutathione) AChe Inhibitors, organophosphates: Atropine > pralidoxime Amphetamines: NH4Cl (acidify urine) Antimuscarinic/anticholinergic: Physostigmine salicylate, control hyperthermia Benzodiazepines: Flumazenil Beta blockers: glucagon CO: 100% O2, hyperbaric O2 Copper, arsenic, gold: penicillamine Cyanide: nitrate + thiosulfate, hydroxocobalamin Digitalis (digoxin): Anti dig Fab fragments Heparin: Protamine sulfate Iron: Deferoxamine, deferasirox Lead: EDTA, dimercaprol, succimer, penicillamine Mercury, arsenic, gold: Dimeraprol (BAL), succimer methanol/ethylene glycol (antifreeze): Fomepizole > ethanol, dialysis Methemoglobin: methylene blue, vitamin C Opiods: naloxone, naltrexone Salicylates: NAHCo3 (alkalinize urine), dialysis TCAs: NaHCO3 (plasma alkalinize) tPA, streptokinase, urokinase: Aminocaproic acid Warfarin: Vitamin K (delayed) FFP (immediate)

What do these groups of drugs cause? Cocaine, sumatriptan, ergot elkaloids Vancomycin, adenosine, niacin, Ca channel blockers Anthracyclines (doxorubicin, daunorubicin); prevent with dexrazoxane Class III and Class IA antiarrythmics, macrolides, antipsychotics, TCAs

What drugs cause coronary vasospasm? Cutaneous flushing? Dilated Cardiomyopathy? Torsades de Pointes?

Reverse pharmacology Flashcards

(47 cards)