M agonist

Chlinesterase inhibitor

M antagonist

Ganglionic blocker

Glaucoma

Pilocarpine

-contract ciliary muscle, pull on trabecular meshwork to relieve pressure

GI/GU

Carbachol

-contracts ureteral smooth muscle

Pulmonary

Bethanechol

-bronchoconstrict

Xerostomia

Pilocarpine(salagen)

-FDA approved for xerostomia assoc w/ head and neck radiation

-5mg tid.

-Thalf-1hr. peaktime 1hr

Cevimeline(evoxac)

-tx for sjogren’s syndrome (1% population w/ female predominate)

-higher affinity for M3 salivary receptor. Minor effect on M2 on heart and eye (palpitation, eye pain)

-increase effect w/ inhibitor of cytochrome P450 enzymes (diltiazem, erythromycin, ketoconazole)

-30mg Thalf-5hrs. peak at 2 hrs

M agonist drug contraindication:

1)COPD (bronchoconstrict)

2)biliary tract disease (contraction of biliary smooth muscle w/ severe abdominal pain)

3)cardiac disease (neg chronotropic, ionotropic, arrthmia, hypotension, AV block)

4)retinal detachment (miosis)

5)renal colic disease (ureteral contraction

6)iritis

side effects:

-flushing, redness

-CNS-confusion, nausea, tremor, vomiting, visual disturbances

Glaucoma

Physostigmine

-competitive blocker, degrade by cholinesterase at slow rate

-tertiary amine, penetrates CNS, good for topical use

Isoflurophate

-irreversible inhibitor

GI/GU

Neostigmine

-also used for myasthenia gravis

-slow bladder and colon function

-side effect: tightness of chest, SOB, increase salivation

Myasthenia gravis

Neostigmin

-inject intramuscularly to avoid central effect

Edrophonium (for dx)

-tx supraventricular tachyarrhythmias

-reversible blocker used as adjunct w/ atropine to counteract it

Alzheimer’s

excessive B amyloid protein, deficiency in CNS Ach

Tacrine (Cognex)

-no improvement in cognitive state, but w/ GI side effect, liver toxicity

Donepezil (Aricept)

-cause death by respiratory failure, diaphragm paralysis

-bronchoconstrict w/ increase mucin secretion

Nicotinic agonist:

-nicotine

-activates para and symph @ ganglionic synapse. Most sym action via epi from adrenal medualla. Initial in crease in BP then decrease

-Para action on increase GI motility and Urinary tract contraction, cramps. Muscle paralysis following contraction

-CNS-convulsion, tremor, depression

Nicotinic antagonist:

Curare

Succinylcholine

-both blocks at neuromuscular junction

Motion sickness

Scopolamine (central acting)

-causes twilight sleep

-29-66% xerostomic effect

mydriatic, cycloplegics (central acting)

atropine

scopolamine

Parkingson’s (central acting)

Benztropin (cogentin)

Counteract neuroleptic drug (phenothiazine)

-decrease excess Ach in basal ganglion neuron

-blurry vision, and drowiness, need to give caution

Trihexyphenidyl (artane)

-also for huntington’s, spastic torticollis

-suppresses perspiration, caution about ambient T

L Dopa (COMT inhibitor), peripheral decarboxylase inhibitors

GI

antispasmatic-for peptic ulcer, GI disorder

Glycopyrrolate (Robinul)

-CI-obstructive uropathy, ulcerative colitis, myasthenia gravis, glaucoma

Propantheline (ProBanthine)

-unlabelled use-for xerostomia prior to dental appt, safer than atropine, no central effect

-15mg (30mg), half hr (1 hr) prior appt

-geriatric, debilitated person need half dose. T-half 9hr

Urinary incontinence

Oxybutynin

Detrol

-for overactive bladder. Decrease bladder smooth muscle contraction

COPD

Ipratropium (Atrovent)

Bronchodilator for asthma, COPD, rhinorrhea assoc w/ cold

-CI: hypersensitivity to atropine

-adm by inhalation, not for tx of acute asthmatic attack.

-rinse mouth after each puff to min xerostomia

Mushroom poisoning

Atropine (sal tropine)

-competitive inhibitor

-antispasmatic, antiarrhythmic, antisialagogue, cyclopegia, antidote for cholinergic crisis (organophosphate poisoning, life threatening bradycardia)-increase 5-10 bt/min by blocking para effect on heart

-0.4mg (1 Tab 1hr prior appt on empty stomach) 4-6 hrs duration

Antihistamine

Diphenhydramine(benadryl)
-blocks H1 receptor

-take 2 25mg cap 1hr prior appt. not as powerful as atropine like drugs. Less side effects. But sedation

Hypertensive emergencies

-block both para and sym

-more effect on sym cuz nicotinic receptors are faster acting, so antagonized 1^st. -produce orthostatic hypotention, decrease GI motility

Trimethaphan

-peripheral effect only

-tx for malignant hypertension

Hexamethonium

Mecamylamine

-rarely used w/ central and pheripheral effect

Pirenzepine

-block M1 receptor, decrease HCl secretion

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M antagonist contraindication:

-narrow angle glaucoma

-cardia, hepatic disease

-urinary, biliary obstruction

-prostate hypertrophy

side effects:

-decrease perspiration and heat loss can lead to hyperexia

-drowsy, nausea, dizzy, xerostomia

-increase HR by unrivalling sym effect on heart