CHAP 5.0 Flashcards by Jan Andrew Pedregosa

General term for agents that bind to cholinoreceptors and prevents the effects of acetylcholine and other cholinergic agonist

Cholinoceptor antagonist

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-also known as antimuscarinic agents or parasympatholytics
-selective blockers of muscarinic receptors

anticholinergic agents

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antagonist on muscarinic receptor

anticholinergic agents

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prototype of antimuscarinic drugs

atropine

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other name of atropine

hyoscyamine

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sources of atropine

Atropa belladona - Deadly nightshade
Datura stramonium - jimsonweed/jamestown weed; sacred datura or thorn apple
Datura metel

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local source of atropine

Datura metel - Talumpunay

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Atropine MOA

bind to muscarinic receptor thereby blocking acetylcholine and other cholinomimetic drugs

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duration of action of atropine

4 hrs except when placed topically in the eye, where action may last for days

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effect of atropine in eye

-mydriasis (dilate pupils)
-reduce lacrimation

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meaning of belladona in italian

beautiful lady

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cosmetically and account for the name bella donna

atropine

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refers to weaken contraction of ciliary muscles
-results in loss of ability to accomodate; the fully atropininzed eye cannot focus for near vision

cycloplegia

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atropine is contraindicated in

glaucoma

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refers to dry mouth

xerostomia

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effect of atropine in GI tract

-xerostomia
-reduced pepsin, acid and mucin
-decreased motility (antispasmodic)
-intestinal paralysis

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anticholinergic drug widely used in diarrhea

loperamide,buscopan

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combination of atropine and diphenoxylate

Lomotil

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effect of atropine in Cardiovascular system

bradycardia = low dose
tachycardia = high dose

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effect of atropine in respiratory system

bronchodilation and reduce secretion

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effect of atropine in genitourinary tract

relaxes smooth muscles, urinary retention

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effect of atropine in sweat glands

-supresses thermoregulatory sweating
-atropine fever
-not recommended for hyperhidrosis

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effect of atropine in CNS

-minimal stimulant at normal dose
-sedative at higher dose

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clinical application of atropine

-mydriatic and cycloplegic agent
-antiplasmodic
-treatment of bradycardia
-antisecretory agent used before surgery
-antidote for cholinergic agonists poisoning

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adverse effects of atropine

-dry mouth -blurred vission -"sandy eyes" -tachycardia -urinary retention -constipation -CNS effects -reverse dumbels

antidote for atropine toxicity

cholinergic agonist (low doses of cholinesterase inhibitors, such as physostigmine)

contraindications of atropine

-glaucoma -prostatic hyperplasia

source of scopolamine

Hyoscyamus niger or henbane

has greater effect on CNS compared to atropine

scopolamine

one of the most effective anti motion sickness drug

scopolamine

can cause short term memory block, sedation, excitement at higher doses, may produce euphoria and is susceptible to abuse

scopolamine

drugs for respiratory disorders

ipratropium tiotropium

a synthetic analog of atropine, is used as inhalational drug in asthma and COPD

ipratropium

has longer broncodilator action and can be given once daily

Tiotropium

The only (dati) anticholinergic used in COPD and asthma

ipratropium

-used to relieve bladder spasm after urologic surgery -also valuable in reducing involuntary voiding in patients with neurologic disease

oxybutinin

a nonselective agonist, has been approved and is comparable in effecacy and side effects of oxybutinin

trospium

anticholinergic that has the advantage of once daily dosing

darifenacin and solifenacin

used for urinary incontinence

tolterodine and fesoteridine

-a tricyclic antideppresant -strong muscarininc functions -has long been used to reduce incontinence -for children with enuresis

Imipramine

a newer antimuscarinic drug approved to reduce incontinence in elderly patients

propiverine

Junction between one neuron to another

Ganglion

Neurotransmitters in ganglion

Acetylcholine

Receptor most likely present in ganglion

Nicotinic receptor

Ganglionic blockade at HIGH DOSE

Nicotine

First nicotinic antagonist recognized

Tetraethylammonium (TEA)

Drug first used for highblood however not common in Ph

Hexamethonium

“C10” depolarizing neuromuscular blocking agent

Decamethonium

Developed because there are problems with other drugs when it comes to absorption via GI tract. Can be absorbed orally.

Mecamylamine

Can be given to patient with nicotine addiction as an adjunct

Mecamylamine

SHORT acting ganglion blocker Inactive orally and give through IV infusion. For hypertensive emergency and dissecting aortic aneurysm

Trimethaphan

BP for hypertensive emergency

>180/125 w/ end organ damage

BP >180/125 WITHOUT organ damage

Hypertensive urgency

MOA of ganglionic blocker

Block ganglionic nicotinic receptors preventing acetylcholine to bind and activate

Prevention of motion sickness and postoperative Nausea and vommiting -pwede sad Vertigo

Scopolamine

Dicyclomine other term

Dicycloverine

Competitive antagonist at M3 receptor

Dicyclomine/loperamide

Reduced smooth muscle and secretory activity of the gut

Effect of dicyclomine

CA: irritable bowel syndrome, minor diarrhea

Dicyclomine

Anticholinergic for diarrhea or spasm

-Dicycloverine -Hyoscyamine-longer duration -Glycopyrrolate - similar to dicyclomine

Competitive antsgonist at all M receptors

Atropine

Effect: mydriasis and cyclopegia

CA: retinal examination CI: glaucoma

Given to asthma and COPD

Ipratropium

Relax brocnhospams

Ipratropium

For urinary incontinence

Oxybutinin

Treatment for cholinergic poisoning

Atropine

Mandatory antidote for severe cholinesterase

Atropine

Antidote for early stage cholinesterase inhibitors poisoning

Pralidoxime

Regenerate AcH

Pralidoxime

Characterized by early signs of muscarinic receptors

Mushroom poisoning

Effect of mushroom

Excessive DUMBELS

Treatment for mushroom poisoning

Atropine

Mushroom that cause delayed onset

Amanita phalloides, A. Virosa, Galerina autumnalis, G marginata

Block cholinergic transmission between motor nerve endings and nicotinic receptors on the skeletal muscle

Neuromuscular agents

2types of neuromuscular blocking agents

Nondepolarizing (competitive) blockers and depolarizing agents

Nondepolarizing blockers

-CURARE -tubocurarine -atracurium>cisatracurium -pancuronium -rocuronium -vecuronium

MOA of nondepolarizing

Low dose- block Ach at nicotinic receptors found at skeletal muscle (muscle relaxants) High dose- blockage of ion channels of motor endplate

Employed by anesthesiologist to shorten duration and monitor the extent of NM blockade

Nondepolarizing agents

Actions of nondepolarizing agents

Paralyze muscles (recover in reverse manner)

Last to relax in paralyzed muscles

Diaphragm

Adverse effect of nondepolarizing agent

Pancuronium- increase heart rate

Agent with actions similar to Ach

Depolarizing agent (more positive inside cell)

Difference between depolarizing agent and Ach

Depolarizing agent in resistant to acetylcholinesterase

Only depolarizing muscle relaxant as of today

Succinylcholine

MOA succinylcholine

Bind to nicotinic receptors and act like ACh

Enzyme degrade succinylcholine

Pseudocholinesterase

Therapeutic use of succinylcholine

-Rapid endotracheal intubation before anesthesia -electroconvulsive shock treatment (correct nerves)

Drug of choice for malignant hyperthermia

Dantrolene

Increase in potassium

Hyperkalemia

Means “no breathing”

Apnea