AChE inhibtors - drugs - toxicity - treatment

- Edrophonium, Physostigmine, Neostigmine, Pyridostigmine, Donepezil, Tacrine, organophosphates - DUMBBELSS (diarrhea, urination, miosis, bradycardia, bronchoconstrict, excitation (CNS/muscle), lacrimation, salivation, sweating - atropine (muscarinic) and pralidoxome (regeneration of AChE)

Antimuscarinics - drugs - toxicity - treatment

- Atropine, TCA, antipsychotics, quinidine, amantadine, merepidine - blind as a bat, mad as a hatter, dry as a bone (mydriasis and cycloplegia, hyperthermia, tachycardia, sedation, urinary retention, constipation, hallucination) - symptomatic and physostigmine

Alpha 1 agonists - MOA - drugs - effect

- increase phospholipase C--> increase IP3, DAG, and Ca2+ (Gq coupled) - phenylephrine, methoxamine - increased TPR, increased BP, potential reflex bradycardia, no change in pulse pressure

Autonomic System Drugs Flashcards by Elizabeth Magowan

Hemicholinium

inhibits choline uptake

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Botulinum toxin

prevents ACh release

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AChE inhibitors

prevent ACh breakdown

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Bethanechol

Muscarinic Agonist
Rx for ileus and urinary retention
- acts on M receptors

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Methacholine

Muscarinic Agonist
Dx of bronchial hyperreactivity
- works on M>N receptors

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Pilocarpine

Muscarinic Agonist

Rx for glaucoma (topical) and xerostomia

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Edrophonium

AChE inhibitor, short acting
Dx of myasthenia
- differentiate from cholinergic crisis

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Physostigmine

AChE inhibitor, tertiary amine (enters CNS)
Rx of glaucoma
antidote for atropine OD

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Neostigmine, pyridostigmine

AChE inhibitor, quaternary amine (no CNS)

Rx of ileus, urinary retention, myasthenia, reversal of nondepolarizing NM blockers

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Donepazil, tacrine

AChE inhibitor, lipid soluble (CNS penetration)

Rx of Alzheimers

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Organophosphates

AChE inhibitor, lipid soluble irreversible
Rx for glaucoma
used in nerve gas and insecticides

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AChE inhibtors

drugs
toxicity
treatment

Edrophonium, Physostigmine, Neostigmine, Pyridostigmine, Donepezil, Tacrine, organophosphates
DUMBBELSS (diarrhea, urination, miosis, bradycardia, bronchoconstrict, excitation (CNS/muscle), lacrimation, salivation, sweating
atropine (muscarinic) and pralidoxome (regeneration of AChE)

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Atropine

Muscarinic Receptor Antagonist

- Rx for antispasmodic, antisecretory, manage AChEi OD, antidiarrheal, ophthamology

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Antimuscarinics

drugs
toxicity
treatment

Atropine, TCA, antipsychotics, quinidine, amantadine, merepidine
blind as a bat, mad as a hatter, dry as a bone
(mydriasis and cycloplegia, hyperthermia, tachycardia, sedation, urinary retention, constipation, hallucination)
symptomatic and physostigmine

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Tropicamide

Muscarinic Receptor Antagonist

- ophthalmology (topical)

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Ipatropium

Muscarinic Receptor Antagonist

- asthma, COPD, no CNS entry

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Scopolamine

Muscarinic Receptor Antagonist

- motion sickness, sedation, short-term memory block

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benztropine, trihexyphenidyl

Muscarinic Receptor Antagonist, lipid soluble, penetrates CNS
- Rx for Parkinsonism and EPS

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Nicotinic Receptor blockers

not really used, work as ganglionic blockers

hexamethonium and mecamylamine
prevent baroreceptor changes in HR (don’t prevent direct drug effects on HR)

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Alpha 1 agonists

MOA
drugs
effect

increase phospholipase C–> increase IP3, DAG, and Ca2+ (Gq coupled)
phenylephrine, methoxamine
increased TPR, increased BP, potential reflex bradycardia, no change in pulse pressure

Phenylephrine

alpha 1 agonist

- Rx for nasal decongestant and mydriasis without cycloplegia

Methoxamine

alpha 1 agonist

- Rx for paroxysmal atrial tachycardia

Alpha 2 agonists

MOA
drugs
effect

decrease adenyl cyclase–>decrease cAMP (Gi coupled)
clonidine, methyldopa
stimulate prejunctional receptors in CNS -> decrease sympathetic outflow (used in mild-mod HTN)

Clonidine

alpha 2 agonist

- Rx for mild-mod HTN

Methyldopa

alpha 2 agonist | - Rx for mild-mod HTN

Beta agonist - MOA - drugs (beta 1/2 and selective beta 2) - effects

- increase adenyl cyclase-->increase cAMP (Gs coupled) - isoproterenol, dobutamine - selective beta 2: salmeterol, albuterol, terbutaline (all for asthma) - beta 1: increased HR, SV, CO, and pulse pressure - beta 2: decreased TPR and BP

Isoproterenol

beta agonist (1 = 2) - bronchospasm, heart block, bradyarrhythmias - SE: flushing, angina, arrhythmia

Dobutamine

``` beta agonist (1 > 2) - CHF ```

Salmeterol, albuterol, terbutaline

beta 2 agonist | - asthma

Ritodrine

beta 2 agonist | - premature labor

Norepinephrine

alpha 1 and 2, beta 1 agonist - no effect on beta 2 - alpha 1: increased TPR and BP - beta 1: increased HR, SV, CO - potential reflex bradycardia - Rx for cardiac arrest, hypoTN

Epinephrine | - low and high dose

alpha 1 and 2, beta 1 and 2 agonist - low dose: beta 1 and 2 stim (increased HR, SV, CO, and PP; decreased TPR and BP) - high dose: alpha 1 and beta 1 stim (increased TPR and BP; increased HR, SV, CO, and PP) - Rx for cardiac arrest, hypoTN, anaphylaxis, asthma

MAO

A: anywhere (mainly in liver), metabolizes NE, 5HT, and tyramine B: mainly in brain, metabolizes DA

Indirect-acting Adrenergic Receptor Antagonist (releasers) - effect - drug interaction - drugs

- displaces NE from mobile pool, only affect SANS - drug interaction by MAO-A (increased bioavailability->HTN crisis) - tyramine, amphetamine, ephedrine

Indirect-acting Adrenergic Receptor Antagonist (reuptake inhibitors) - effect - drugs

- inhibit reuptake | - cocaine, TCA

alpha receptor antagonists - effect - use - drugs

- decrease TPR and mean BP, may cause reflex tachycardia and Na/H2O retention - HTN, pheochromocytoma (nonselective), BPH (selective alpha1) - nonselective or selective

Nonselective alpha blocker - use - drugs

- pheo | - phentolamine (competitive) and phenoxybenzamine (non-competitive)

selective alpha1 blocker - use - drugs

- BPH | - prazosin, doxazosin, terazosin, tamsulosin

selective alpha2 blocker - use - drugs

- yohimbine (postural hypoTN and impotence) | - mirtazapine (antidepressant)

Beta1 blocker

- decrease HR, SV, and CO, decrease renin release, decrease aqueous humor release

Beta2 blocker

- bronchospasm and vasospasm, block gluconeogenesis and glycogenolysis-->increase LDL and TG

Antiarrhythmic beta blockers

propranolol, acebutolol, esmolol

timolol

- beta blocker | - Rx for glaucoma

propranolol

- beta blocker | - migraine, thyrotoxicosis, performance anxiety, essential tremor

sotalol

- K+ channel blocker and beta blocker

labetolol and carvedilol

- alpha1 and beta blocker | - use in CHF

Glaucoma (open angle) - description - Tx

- increased IOP due to decreased resorption - beta blockers-->decrease aqueous production - muscarinic activators-->improve drainage

Glaucoma (closed angle) - description - Tx

- acute (painful) with increased IOP due to blocked canal of Schlemm - cholinomimetics, carbonic anhydrase inhibitors, mannitol (antimuscarinics and alpha1 agonists are contraindicated)

Tx for glaucoma - pilocarpine - echothiophate - timolol

- cholinomimetic-->activate M receptors-->contract ciliary muscle-->increase flow through canal - AChEi-->increased outflow - block NE-->decrease humor formation