Midterm Chapter 5 Cholinergic Antagonist Flashcards by KENNETH ESPALABRA

General term for AGENT THAT BIND TO CHOLINOCEPTORS and PREVENT THE EFFECT OF ACETYLCHOLINE and other cholinergic agonist

Cholinoceptor Antagonists

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Selective blockers of Muscarinic receptors

Anticholinergic Agent

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also known as “Antimuscarinic agent or “muscarinic receptor”

Anticholinergic Agent

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affinity to muscarinic receptor but no intrinsic activity

anticholinergic Agent

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also known as “hyoscyamine”

Atropine

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Prototype of Antimuscarinic Drug

Atropine

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Plant Source:
English Name- (Scientific Name)
deadly Nightshade- (SCIENTIFIC NAME)
Jamestown weed/jimsonweed.sacred datura/thorn apple- (SCIENTIFIC NAME)
local Source:

Talumpunay - (SCIENTIFIC NAME)

Plant Source:
English Name- (Scientific Name)
deadly Nightshade- (Atropa belladona)
Jamestown weed/jimsonweed.sacred datura/thorn apple-(Datura stramonium)

local Source:
Talumpunay - (Datura metel)

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NOTE AND EXPLANATION!

MOA of Atropine:
Causes reversible (summountable(overcome)) blockade of cholinomimetic action at muscarinic receptor

In short:
its MOA it binding to muscarinic receptor thereby blocking the effects of acetylcholine and other cholinomimetic drug, mag bind lang siya, pero walang activation, walay dUMMBELLS mahitabo

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ACTION OF ATROPINE:

Action last about ___ hours except when
Topically in the eye, where the action may last for _____

Action last about 4 hours except when
Topically in the eye, where the action may last for days

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AFFECT OF ATROPINE IN SPECIFIC ORGAN

EYE
GASTROINTESTINAL TRACT
CARDIOVASCULAR SYSTEM
RESPIRATORY SYSTEM
GENITOURINARY TRACT
SWEAT GLANDS
CENTRAL NERVOUS SYSTYEM

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NOTE ONLY!
EYE:
-Mydriasis
-cycloplegia
-cannot focus for near vision
-contraindicated in glaucoma
-Reduce lacrimation -“dry or sandy eyes”

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an Italian term means “beautiful lady”

belladona

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it means weaken contraction of the ciliary muscle

cycloplegia

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it means to dilate pupil cosmetically and was name belladonna

Mydriasis

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NOTE ONLY!
Gastrointestinal tract
-Xerostomia
-Pepsin, acid and mucin- reduce volume and amount
-antispasmodic
-decrease motility-intestinal paralysis
-now rarely used for peptic ulcer
-lomotil (r) = Atropine + diphenoxylate =treatment for Traveler’s Diarrhea and hypermotility treatment

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NOTE ONLY!
Loperamide and Buscopan is also a anticholinergic drug

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lomotil(r) is now reformulated and was name in today as…..

loperamide

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it means dry mouth

Xerostomia

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it means to relax muscle spasm and cramps

Antispasmodic

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lomotil (r)= atropine + _________

diphenoxylate

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NOTE ONLY!
Cardiovascular
-has little effect on Blood pressure
-Bradycardia- lowdose
-tachycardia-highdose

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Bradycardia low doses - has____ ____ beats per minutes

has less 60 BPM

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Tachycardia high doses - has____ ____ beats per minutes

has exceed 100 BPM

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Normal Heart rate

60-100 BPM

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High dose effect of Atropine in Cardiovascular System?

Tachycardia

Low dose effect of Atropine in Cardiovascular System?

Bradycardia

Note Only! Resperatory System-Atropine -Bronchodilation -Used in Asthmatic and COPD Patients

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Respiratory System can cause ——-, in response to Atropine

Bronchodilation

Note Only! GenitoUrinary Tract -Relaxes smooth Muscles of the ureters and bladder wall -Urinary retention

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Inability to empty the bladder completely

Urinary retention

Note Only! Sweat Glands -Suppresses thermoregulatory sweating -block the nerve signals that stimulates sweating -“atropine fever” -Hyperhidrosis(Apocrine glands)

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It means excessive sweating

Hyperhidrosis

Sweat Glands: Effect of atropine in infant and children at ordinary dose

Atropine fever

What does atropine does to sweat glands?

Supresses thermoregulatory sweating

In Sweating, Which gland does armfit and genital belong?

Apocrine gland

In Sweating, Which gland does the “all over the body” belong to?

Eccrine Gland

Note only! Effect of Atropine in CNS:( Normal Dose) - Minimal Stimulant on CNS -Sedative effect, slower, longer lasting on the brain

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Antidote for cholinergic agonist poisoning

Atropine

Antidote for atropic toxicity

Physostigmine

Two Contraindication of Atropine

-Glaucoma -Prostatic Hyperplasia

Note Only! Clinical Application of Atropine( Used for) -Mydriatic and cycloplegic agent -antispasmodic -Treatment for bradycardia -antisecretory agent used before surgery -antidote for cholinergic agonist poisoning

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Note Only! Adverse effect of Atropine:(Side Effect) -Dry Mouth -Blurred vision -Sandy Eye -Tachycardia -urinary retention -Constipation -CNS Effect

-….

Scopolamine is also known as..

Hyoscine

Greater action in CNS than atropine

Scopolamine

Plant Source of Scopolamine

Hyoscyamus niger

Anti Motion Sickness Drug

Scopolamine

Common brand of scopolamine

Buscopan (r)

Note Only! Scopolamine = Buscopan(R) -“Hyosine” =Hyoscyamus niger -Greater action in CNS than Atropine -Anti-Motion Sickness Drug -Sedation/Sedative -High Dose- Euphoria and susceptable to abuse THERAPEUTIC USES: -Motion sickness (Topical Patch -3days) -Postoperative nausea and vomiting

Drugs for Respiratory Disorders:

IpraTROPIUM TioTROPIUM

Longer bronchodilators Action (Once Daily)

Tiotronium

Synthetic Analog of Atropine

Ipratronium

Inhalation drug in Asthma and COPD

Ipratronium

Ipratronium and Tiotronium is an example of……

Relaxant of Bronchial Smooth Muscle (BRONCHODILATORS)

Other Antimuscarinic Drug

-Oxybutinin= Ditropan (R) -Trospium -DariFENACIN and SoliFENACIN -TolTERODINE and FesoTERODINE -Imipramine -Propiverine

Relieve blader spasm after prostatectomy Reducing involuntary voiding in patient with neurological disease

Oxybutinin

Brand name of oxybutinin

Ditropan (R)

Nonselective antagonist

Trospium

Also comparable to SE and efficacy of oxybutinin

Trospium

Advantage of once- Daily dosing

DariFENACIN and SoliFENACIN

Adult with urinary Incontinence

TolTERODINE and FesoTERODINE

Tricyclic Antidepressant

Imipramine

Strong Antimuscarinic Function

Imipramine

LONG been use to reduce incontenence in INTITUTIONAL ELDERLY PATIENTS

Imipramine

NEWER ANTIMUSCARINIC DRUG approved to reduce incontinence in elderly patients

PROpiverine

Note Only! Basic & Clinical Pharmacology of the Ganglion-Blocking Drugs: -Nicotine -Tetraetylammonium (TEA) -Hexamethonium (Hypertention) -Decamethonium (Carbon 10) -Mecamylamine -Trimethaphan

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COMPETITIVELY BLOCK the action of acetylcholine and similar agonists at nicotinic receptors of both parasympathetic and sympathetic autonomic ganglia

Ganglion- Blocking drug

More Positive Inside the Cell (Na+) (More Active) that causes CNS stimulant

Depolarization

•Low dose – depolarizes autonomic ganglia – stimulation •High dose – ganglionic blockade – blood pressure falls and GIT & bladder musculature ceases

NICOTINE

Nicotine: Effect: ganglionic blockade – blood pressure falls and GIT & bladder musculature ceases

High Dose

Nicotine: Effect: depolarizes autonomic ganglia – stimulation

Low Dose

First to recognized (Ganglion Blocking Drug) but VERY SHORT DURATION

Tetraethylammonium (TEA)

First drug effective for management of HYPERTENSION

Hexamethonium

DEVELOP TO IMPROVED and Extend absorption from GI due to Quarternary amine ganglion Secondary Amine

Mecamylamine

DEVELOP AND INTRODUCED clinically First drug effective for management of HYPERTENSION

Hexamethonium

“C10” analog of hexamethonium

Decamethonium

Blocking compound were poorly and erratically absorbed after oral administration

Quarternary Amine ganglion

Nicotine patch to reduce smoking cravings

Mecamylamime

Depolarizing neuromuscular blocking agent

Decamethonium

SHORT ACTING ganglion blocker

Trimethaphan

Inactive orally, given via IV infusion

Trimethaphan

Hypertensive emergencies and dissecting aortic aneurysm

Trimethaphan

MOA: unknown MOA in CNS Effects: Reduces vertigo, post-operative nausea CA: Prevention of motion sickness and postoperative N & V

Scopolamine

MOA: competitive antagonist at M3 receptor Effects: Reduces smooth muscle and secretory activity of the gut CA: Irritable bowel syndrome, minor diarrhea

DICYCLOMINE (Bentyl®)

longer duration of action

HYOSCYAMINE

- similar to dicyclomine

GLYCOPYRROLATE

MOA: competitive antagonist at all M receptors Effects: mydriasis and cycloplegia CA: Retinal examination CI: Glaucoma

ATROPINE

MOA: Competitive, non-selective antagonist at M receptors Effects: Reduces/prevents bronchospasm CA: Prevention & relief of acute episodes of bronchospasms

IPRATROPIUM (Atrovent)

MOA: non-selective muscarinic antagonist Effects: Reduces detrusor smooth muscle tone, spasms CA: Urge incontinence, post-operative spasms

OXYBUTININ (Ditropan®)

mandatory antidote for sever cholinesterase inhibitor poisoning

Atropine

MOA: very high affinity for phosphorus atom but does not enter CNS Effects: Regenerates active AChE; can relieve skeletal muscle and plate block CA: Usual antidote for early stage (48hrs) cholinesterase inhibitor poisoning

PRALIDOXIME (Protopam)

•Pralidoxime (PAM) and diacetylmonoxime (DAM) given IV •not recommended for poisoning caused by carbamates

Cholinesterase Regenerator Compounds

(PAM) and (DAM) means

Pralidoxime (PAM) and diacetylmonoxime (DAM

characterized by early signs of muscarinic excess

Muschroom poisoning

- apparent within 30 mins to 2 hrs after ingestion

Rapid -Onset Type

apparent within 30 mins to 2 hrs after ingestion muschroom poisoning antidote?

Atropine

Delayed-onset - usually caused by -Amanita phalloides, -A virosa, - Galerina autumnalis, -G marginata

Mushroom Poisoning Delayed-onset - usually caused by Amanita phalloides, A virosa, Galerina autumnalis, G marginata - first symptoms: 6-12 hours after ingestion - major toxicity involves hepatic and renal cellular injury - Atropine is of no use in this form of mushroom poisoning

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

NEUROMUSCULAR BLOCKING AGENTS

NEUROMUSCULAR BLOCKING AGENTS TYPES

Nondepolarizing (competitive) blockers – antagonist Depolarizing agents – agonist

Notes only! NONDEPOLARIZING BLOCKERS: •Curare •Tubocurarine •Atracurium  Cisatracurium •Pancuronium •Rocuronium •Vecuronium

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Mechanism of Action •Low dose – competitively block ACh at the nicotinic receptor (reversed by cholinesterase inhibitors, i.e. neostigmine) – employed by anesthesiologist to shorten the duration and monitor the extent of NM blockade High dose – block the ion channels of the motor endplate – cannot be reversed by cholinesterase inhibitors – results to complete blockade, thus the muscles do not respond to direct electrical stimulation anymore

Actions Sequence of paralyzed muscles: •Small, rapidly contracting muscles of the face and eyes are most susceptible •Fingers, limbs, neck, trunk muscles, intercostal muscles •Diaphragm ** recovery follows the reverse manner Adverse Effects •Pancuronium – increased heart rate

Drug Interactions •Cholinesterase Inhibitors •Halogenated hydrocarbon anesthetics •Aminoglycoside antibiotics •Calcium channel blockers

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DEPOLARIZING AGENT •Works by depolarizing the plasma membrane of the muscle fiber, similar to the action of ACh •Resistant to degredation by AChE •SUCCINYLCHOLINE – only depolarizing muscle relaxant in use today

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Mechanism of Action •Attaches to the nicotinic receptors and acts like ACh Phase I - causes the opening of Na channel which results to depolarization of the receptor (transient twitching of the muscle or fasciculation) Phase II – continuous depolarization gives way to gradual repolarization as the Na channel closes or is blocked (flaccid paralysis) Actions •Initially produces brief muscle fasciculations causing muscle soreness •Respiratory muscles are paralyzed last •DOA – extremely short due to pseudocholinesterase

Therapeutic Uses •Useful for rapid endotracheal intubation required during induction of anesthesia •Electroconvulsive shock treatment Adverse Effects •Malignant hyperthermia – antidote: Dantrolene •Apnea •Hyperkalemia

Malignant hyperthermia – antidote:——

Dantrolene

Midterm Chapter 5 Cholinergic Antagonist Flashcards

(105 cards)