Reverse pharmacology Flashcards
Direct cholinnomimetic agonist
Postoperative ileus, neurogenic ileus, urinary retention
Activates bladder and bowel smooth muscle
bethanacol
Direct cholinomimetic agonist
Constricts pupil and relieves intraocular pressure in glaucoma
carbachol
Direct cholinomimetic agonist
challenge test for diagnosis of asthma
methacholine
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
Anticholinesterases (3)
Alzheimers
donezipil, galantamine, and rivastigmine
Anti AChE
Historically, diagnosis of myasthenia gravis (extremely short acting)
edrophonium
Anti AChE
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockage
No CNS penetration
neostigmine
Anti AChE
Anticholinergic (atropine) toxicity; crosses blood rain barrier
physostigmine
Anti AChE
Myasthenia gravis (long acting)
No CNS penetration
pyridostigmine
Muscarinic antagonists (3)
Mydriasis and cycloplegia
atropine
homatropine
tropicamide
Muscarinic antagonists
Parkinsons
Acute dystonia
Benztropine
Muscarinic antagonists
Parenteral: Pre op use to reduce airway secretions
Oral: Drooling, peptic ulcer
glycopyrrolate
Muscarinic antagonists (2)
Antispasmodics for irritable bowel syndrome
hyoscyamine
dicyclomine
Muscarinic antagonists (2)
COPD, asthma
ipratropium, tiotropium
Muscarinic antagonists (3)
Reduce bladder spasms and urge incontinence
oxybutynin, solifenacin, tolterodine
Muscarinic antagonists
Motion sickness (CNS)
scopolamine
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
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
Reef fish
Opens Na channels causing depolarization
Similar to cholinergic poisoning
Temperature related dysthesias are a specific finding
Supportive
Ciguatoxin
Very potent: binds fast voltage gated Na channels and prevents depolarization
Pufferfish
Nausea, diarrhea, paresthesias, weakness, dizziness, loss of reflexes
Supportive
tetrodotoxin
Direct sympathomimetics
beta 2 > beta 1
Acute asthma
albuterol
Direct sympathomimetics
beta 1 > beta 2
alpha
Heart failure (inotropic > chronotropic) Cardiac stress testing
dobutamine
Direct sympathomimetics
D1=D2 > beta > alpha
unstable bradycardia
HF
Shock
Inotropic and chronotropic alpha effects predominate at high doses.
dopamine
Direct sympathomimetics
Beta > alpha
Anaphylaxis
asthma
open angle glaucoma
Alpha effects predominate at high doses
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)
NE
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?
