• Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

Card Range To Study

through

image

Play button

image

Play button

image

Progress

1/31

Click to flip

Use LEFT and RIGHT arrow keys to navigate between flashcards;

Use UP and DOWN arrow keys to flip the card;

H to show hint;

A reads text to speech;

31 Cards in this Set

  • Front
  • Back
Alpha-Latrotoxin (Black Widow Spider)
Facilitate Spontaneous ACh Release to Excess
Botulinum Toxin aka Botox (Clostridium botulinum)
Mx: Block ACh Release

Causes Flaccid Paralysis

Uses:
1) Wrinkle Reduction
2) Eye Squinting
3) Certain types of Headaches
4) Jaw Clenching
5) Movement Disorders
6) Bladder Spasms
7) Excessive Sweating
Hexamethonium
Preferentially Blocks GANGLIONIC (NN or NG) AChR in Autonomic Ganglia and Adrenal Medulla
d-Tubocurarine aka Tubarine aka Tubadil
Competitive (Non-Depolarizing)

Preferentially Blocks NEUROMUSCULAR (NM) AChR at Neuromuscular Synapses of Somatic System

NOT Completely Selective, and can produce some degree of Ganglionic Blockade, possibly contributing to Hypotensive Effects

Active Ingredient of Curare, Plant from SA

NOT Absorbed Orally due to 2 Quaternary Nitrogen Functions

Duration = 20-40 Minutes

Releases Histamine:
1) Reduces BP
2) Increases Respiratory Secretions
3) Produces some Bronchospasm
4) Increases Salivary Secretion

Sequence of Paralysis:
Small Rapid Muscles (eyes, ears, mouth, fingers, toes) > Limbs, Neck > Intercostal Muscles > Diaphrahm (last)
Cevimeline
Mx: Selective M1 Muscarinic AChR AGONIST

Uses:
1) Treat Dry Mouth in SJOGREN'S SYNDROME
2) Possibly useful in Alzheimer's to reduce symptoms and plaque lesions
Side Effects of Muscarinic Cholinergic AGONISTS
Most Serious:
1) Hypotension
2) Bradycardia
3) Bronchial Constriction
4) Exacerbation of Peptic Ulcers

Most Common: ***"SLUDS" Syndrome***
S = Salivation
L = Lacrimation
U = Urination
D = Defection
S = Sweating

Antidote = ATROPINE!
Methacholine (Mecholyl)
Selective Muscarinic AChR AGONIST (due to β-methyl group)

Resistant to hydrolysis via PLASMA Cholinesterases

Hydrolyzed by Acetylcholinesterases at 1/3 rate of ACh

Uses:
1) Diagnostically to test responses of Bronchial Hyper-reactivty for Asthma
Carbachol (Doryl or Carcholin)
LITTLE Selectivity for AChR Types

Carbamate Substitution in Acetyl Moiety protects it from Hydrolysis from BOTH Plasma Cholinesterases AND Acetylcholinesterases = Long Duration (2-3 Hours)

Uses:
1) Topically in Eye for GLAUCOMA
Bethanechol (Urecholine)
Combines Structural Features of METHACHOLINE (β-methyl group) and CARBACHOL (carbamate substition)

Selective for Muscarinic AChR

Long Duration (2-3 Hours)

Uses:
1) Orally or SC - Increases Tone and Contractions of the Intestine and Urinary Bladder

2) IV or IM - Negates Specificty and Increases Toxicity - DO NOT ADMINISTER THIS WAY
Pilocarpine
Natural Plant Alkaloid

Primarily Muscarinic AChR AGONIST

NOT a Choline Ester
NOT a Substrate for AChE

Long Duration (2-3 Hours)

Uses:
1) Topically in Eye for GLAUCOMA
2) Very Potent actions on Sweat Glands
3) Prominent and Complicated actions on CV
4) Effects in CNS

Thus, NOT used Systemically!
Nicotine
Natural Plant Alkaloid

Central Effects:
1) Mild CNS Stimulant
2) Stimulates Respiration
3) Induces Vomiting

Peripheral Effects:
1) Stimulate Ganglionic NAChR --> Release of NE, leading to:
2) Tachycardia
3) Increase in BP
4) Increased GI Secretions and Motility

Very high doses can block NAChR by inducing persistent Depol.

Thus, effects of Nicotinic Ganglionic Agonists are UNPREDICTABLE = NOT useful for Therapeutics (exception = Varenicline)
Varenicline
Some Selectivity for NN α4β2

Uses:
1) Smoking Cessation/Withdrawl
Physostigmine aka "Eserine"
Reversible (Carbamate) AChE Inhibitor

3 Amine --> Crosses BBB

Natural Plant Alkaloid from Calabar or "Ordeal" Beans from West Africa

Uses:
1) Antidote against Atropine Poisoning
2) Topically in Eye for Glaucoma
3) Possibly improve symptoms of Alzheimer's (Donepezil is a new, more selective alternative)
Neostigmine (Prostigmin)
Reversible (Carbamate) AChE Inhibitor

4 Amine --> Does NOT Cross BBB

Stimulates GI Contractions and Secretions
Stimulates Urinary Contractions
Improves Neurotansmission at Jx of Somatic Nerves and Skeletal Muscle

Uses:
1) Nonobstructive Intestinal and Urinary Bladder Atony
2) Management of MYASTHENIA GRAVIS
Edrophonium (Tensilon)
Reversible (Carbamate) AChE Inhibitor

4 Amine --> Does NOT Cross BBB

Short Duration

Uses:
1) Very Useful for Functional Tests, e.g. Dx of MYASTHENIA GRAVIS
Echothiophate (Phospholine)
Irreversible (Organophosphate) AChE Inhibitor

Long Duration (100 Hours)

Does NOT readily penetrate the Skin and is Stable in Solution (Unique to Organophosphates)

Uses:
1) Topically in the Eye for Glaucoma
Sarin
Irreversible (Organophosphate) AChE Inhibitor

Prototype Military "Nerve Gas" (others include Tabun and Soman)

Crosses the BBB and induces both Central and Peripheral AChE Inhibition.

NOT used as a drug.
Malathion
Irreversible (Organophosphate) AChE Inhibitor

Prototype Organophosphate INSECTICIDE

Because mammals detoxify it readily, large amounts are required to suffer intoxication.
Pralidomide aka Protopam (PAM)
AChE REACTIVATOR

4 Amine --> Does NOT Cross BBB

Treatment for Organophosphate Intoxication must be initiated quickly after exposure. If the P-Enzyme has fully "Aged", it is USELESS.
Pirenzepine
M1 Selective Muscarinic AChR ANTAGONIST

Uses:
1) Inhibitor of Acid Secretion without the normal side effects (PEPTIC ULCER DISEASE)
Tolterodine
M3 Selective Muscarinic AChR ANTAGONIST

Uses:
1) Adults with Urinary Incontinence
2) Bladder Antispasmodic Agent to Inhibit Contractions After Bladder Surgery
Atropine
Non-Selective Muscarinic AChR ANTAGONIST

Natural Plant Alkaloid from Belladonna Plants and Jimson Weed

3 Amine - Can Cross BBB

Half Life = 2-4 Hours

Sx:
1) Eye - Produces Mydriasis (Pupil Dilation) and Cycloplegia (Loss of Accommodation)
2) GI Tract - Reduces Secretions and Motility
3) Decreases Thermoregulatory (Sudomotor) Sweating
4) Mild Tachycardia
5) Bronchial Relaxation
6) ***One Effect NOT related to Muscarinic Blockade***: Dilation of Blood Vessels in Facial Blush Area = ATROPINE FLUSH (Due to DIRECT, NON-Muscarinic Effect on Vascular Smooth Muscle)

Uses:
1) Preanesthetic Medications to reduce salivary/respiratory secretions and to induce amnesia (Scopolamine also can be used).
2) Examination of the Retina and Treatment of Acute Iritis - Topically in Eye to induce Mydriasis and Cycloplegia
3) Treatment of Organophosphate AChE Inhibitor Poisoning

In Children, low dose can Block Sweating --> Increased Temp = "Atropine Fever"

Antidote for Atropine Poisoning = Physostigmine (penetrates CNS)
Scopolamine
Natural Belladonna Alkaloid, Similar to Atropine in many ways

3 Amine --> Can Cross BBB

Differences from Atropine:
1) Exerts MORE CNS Action, especially Drowsiness (Dreamless Sleep - Loss of REM) and Amnesia
2) Antimotion Sickness Agent - Blocks Muscarinic AChRs in Vestibular System and in Brain
Propantheline
Synthetic Muscarinic AChR ANTAGONIST

4 Amine --> Does NOT Cross BBB

Uses:
1) Peptic Ulcer Disease (Pirenzepine is better as it is more specific (M1) and thus less side effects)
Ipratropium (Atrovent)
Synthetic Muscarinic AChR ANTAGONIST

4 Amine --> Does NOT Cross BBB

Uses:
1) Reversible Airway Disease (Tiotropium is a very similar alternative which gives a LONGER bronchodilation)
2) Marginal Benefits to treatment of Common Colds (reduce secretions of Nasopharynx)
What class of drugs is beneficial in the management of Parkinson's Disease?
Muscarinic Recetor ANTAGONISTS!

May be given concomitantly with Levodopa.
Trimethaphan (Arfonad)
The ONLY Clinically Relevant Ganglionic Blocking Drug

Uses:
1) Lower BP Rapidly in Hypertensive Crisis

Side Effects:
1) Constipation (Blockade of Enteric Ganglia)
2) Urinary Bladder Atony
3) Cycloplegia
4) Decreased Sweating
5) Tachycardia (Baroreceptors)
Atracurium (Tracrium)
Competitive (Non-Depolarizing) Motor End-Plate Blockade

Presently Popular
Succinylcholine (Anectine)
Depolarizing Motor End-Plate Blockade

Nicotinic Agonists which produce a Transient Contraction, followed by PERSISTENT Depol and PREVENTED Repol

Intensified with AChEI and by Hypothermia

Ester of TWO Choline Residues w/ Succinic Acid

Short Duration (2-3 Minutes) - usually given by IV Drip

Uses:
1) Adjunct in Surgical Anesthesia - Muscle relaxation while using lower levels of general anesthetic
2) Orthopedic Procedures
3) Intubation (useful due to short duration)
4) Electroshock Therapy

Contraindications:
1) Can Exacerbate Hyperkalemia in patients with Extensive Soft-tissue damage (burn victims)
2) In individuals with Genetic Mutations in Ryanodine Receptor, combination with Halothane leads to widespread muscular rigidity + rapid rise in temp = Malignant Hyperthermia. Treated with Dantrolene (blocks Ca2+ Release)
3) In individuals with Genetic Deficiency causing Reduced Plasma AChE, can cause Prolonged Apnea
Ether and Halothane (volatile anesthetics) interactions with Neuromuscular Blockers
Stabilize a Hyperpolarization of Post-Synaptic Membrane

INCREASE Blockade by COMPETITIVE Blockers (tubocurarine)
Aminoglycosides, Tetracycline, and Certain Peptide Antibiotics (certain antibiotics) interactions with Neuromuscular Blockers
Have Curare-Like Activity

Enhance Blockade by adding their OWN Component!