Drugs of the Cholinergic System Flashcards

Question

Oxybutynin

Answer 1

Antimuscarinic Some M3 Selectivity Use: Urinary Frequency

Answer 2

Antimuscarinic Better M3 Selectivity (than Oxybutynin) Use: Urinary Frequency

Answer 3

Antimuscarinic Better M3 Selectivity (than Oxybutynin) Use: Urinary Frequency

Answer 4

M3 Selective Antimuscarinic Use: Urinary Frequency

Answer 5

Non-Selective Antimuscarinic Use: Urinary Frequency

Answer 6

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker 1) Quaternary Alkaloid 2) No CNS effects @ Therapeutic doses 3) Not well Absorbed after Oral administration (which is why they were able to eat the meat of the animals they had killed with Curare) South American Arrow Poison Active Compound is D-Tubocurarine

Answer 7

Prototype Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker Active compound in Curare 1) Quaternary Alkaloid 2) Not well absorbed with Oral administration 3) No CNS effects @ Therapeutic doses 4) Weak Ganglionic Blocker => Hypotension 5) Liberates Histamine => Hypotension => Bronchospasm (These adverse effects are why we no longer use this)

Answer 8

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker **Broken Down by Hoffman Elimination! => **Temperature and pH Dependent _Not Enzymatic breakdown (Not patient dependent) **Does NOT Depend on Hepatic or Renal Function for its breakdown. _Thus, will last just as long in elderly and healthy younger person. Also Broken Down by Ester Hydrolysis

Answer 9

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker Stereoisomer of Atracurium Produces Less Histamine than Atracurium (Now widely used)

Answer 10

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker Has Steroid structure. Rapid Onset Intermediate Duration May be used to Facilitate Intubation. (Like, need the patient to be paralyzed briefly for just a brief procedure, like intubation)

Answer 11

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker Investigational New class (chemical structure) Ultra-Short-Acting --May be an Alternative to Succinylcholine (which is a Depolarizing blocker and the only other ultra-short-acting blocker available)

Answer 12

Prototype Depolarizing (Partial Agonist) Neuromuscular Blockers 1) Very Brief Duration of Action (5-10 min) 2) Hydrolyzed by Plasma Pseudocholinesterase _____________ May Get Prolonged Action: 1) Severe Malnutrition (Not synthesizing enough Pseudocholinesterase) 2) Hepatic Disease (Not synthesizing enough Pseudocholinesterase) 3) Drug Interactions: _Neostigmine and other Anticholinesterases _Ester Local Anesthetics (Esters are Broken down by Pseudocholinesterase; thus, compete with succinylcholine for enzymatic breakdown) 4) Organophosphate Exposure (Chronic, Sub-Clinical): e.g. Field workers and Avid Gardeners with Chronic, Low-dose use of Insecticides 5) Succinylcholine Apnea: Genetic difference in type of Pseudocholinesterase (less effective form) ``` __________ Diazepam: _Increases Duration of Non-Depolarizing Blockers _Decreases Duration of Succinylcholine (Depolarizing Blocker) ``` ____________ Adverse Effects: 1) Malignant Hyperthermia: Treat with Dantrolene* 2) Hyperkalemia => Results in Cardiac Depression (More common in Burn, Trauma patients; Dangerous if on Digoxin) 3) Histamine Release 4) Ganglionic Block: => Hypotension! 5) Bradycardia: (Muscarinic) _Cardiac Arrest may result 6) Increased Bronchial Secretions (Muscarinic) (Both Succinylcholine and Acetylcholine are derived from Choline. So, may act @ Muscarinic receptors too.) 7) Fasciculations of Abdominal Muscles: Causing Increased IntraGastric Pressure: => Increased Risk for Reflux (Most likely in patients with Delayed Gastric Emptying, e.g. Diabetics, Morbid Obesity 8) Increased IntraOcular Pressure: - -Transient (Peaks @ 2-4 min) 9) Post-Operative Muscle Pain __________________ HOW TO REVERSE EFFECTS: _Give Plasma!! Need Normal Pseudocholinesterase!!! _Cannot give Neostigmine b/c will only exacerbate. _Don't give Atropine because Atropine is a Muscarinic Blocker.

Answer 13

Ganglion Blockers No longer available in USA Uses: _Anti-Hypertensive (Short-term, for Hypertensive Crisis) Adverse Effects: _Many; Depend on the predominant tone at the time of the block _Usually see Decreased Muscarinic Effects: 1) Mydriasis (Dilated Pupils) (Iris) 2) Cycloplegia, Blurred Vision (Ciliary muscle) (Accommodation) 3) Dry Mouth (Xerostomia), 4) Anhidrosis (Sweat Glands) (Sympathetic) 5) Tachycardia 6) Constipation 7) Urinary Retention Note: 1) Predominant Tone in Vasculature is Sympathetic. _Ganglionic Block results in Vasodilation, Hypotension. (Sweat Glands Sympathetic too) 2) Predominant Tone everywhere else is Parasympathetic. _Ganglionic Block results in Anti-Muscarinic effects.

Answer 14

Ganglion Blockers No longer available in USA Uses: _Anti-Hypertensive (Short-term, for Hypertensive Crisis) Adverse Effects: _Many; Depend on the predominant tone at the time of the block _Usually see Decreased Muscarinic Effects: 1) Mydriasis (Dilated Pupils) (Iris) 2) Cycloplegia, Blurred Vision (Ciliary muscle) (Accommodation) 3) Dry Mouth (Xerostomia), 4) Anhidrosis (Sweat Glands) (Sympathetic) 5) Tachycardia 6) Constipation 7) Urinary Retention Note: 1) Predominant Tone in Vasculature is Sympathetic. Ganglionic Block results in Vasodilation, Hypotension. (Sweat Glands Sympathetic too) 2) Predominant Tone everywhere else is Parasympathetic. Ganglionic Block results in Anti-Muscarinic effects.

Answer 15

Inhibits Release of Acetylcholine * Uses (Diluted form): 1) Local Muscle Spasms 2) Excessive Sweating 3) Cosmetic (Reduce Wrinkles) 4) Migraines Extremely Toxic! High Mortality. Recovery: Weeks to Months Food Poisoning => Progressive Parasympathetic Block => Motor Paralysis 1) Dry Mouth, 2) Blurred Vision 3) Difficulty Swallowing 4) Progressive Respiratory Paralysis => Death! Anti-toxin is used to treat the poison.

Drugs of the Cholinergic System Flashcards

(39 cards)