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Anticholinergics

Anticholinergics are a broad class of medications that are involved in many disease and condition states. An Anticholinergic Agent is a substance that works to stop or block Neurotransmitters in the Brain. It inhibits parasympathetic nerve impulses.

Acetylcholine is the substance that is blocked.

These types of drugs can be divided into three Areas

1.)  Antimuscarinic Agents

2.)  Ganglionic Blockers

3.)  Neuromuscular Blockers

*** For our purposes – 2 Classifications will be used.

Medical Uses For Anticholinergics:

Gastrointestinal Disorders

–  Diarrhea
–  Nausea
–  Vomiting
–  Gastritis
–  Ulcerative Colitis
–  Diverticulitis
–  Others

Genitourinary Disorders

–  Cystitis
–  Urethritis
–  Prostatitis

Respiratory Disorders

–  Asthma
–  Acute and Chronic Bronchitis
–  Chronic Obstructive Pulmonary Disease or COPD

Sleeping Disorders

Heart Problems

–  Sinus Bradycardia

Dizziness

–  Vertigo
–  Motion Sickness

There are Two Broad Classifications of these Medication

1.)  Antimuscarinic Medications

Antimuscaranic medications or method of action affects the “muscarinic acetylcholine receptors”

– There is a reduction of action on these receptors

Examples of Antimuscarinic Medications

.  Atropine     Uses:  anesthesia, bradycardia, anticholinesterase overdose or poisoning

Adverse effects: blurred vision, urinary retention

.  Scopolamine      Uses: motion sickness, nausea, cramping

.  Ipratropium brominde  [Atrovent HFA]     Uses: Asthma, Bronchitis, COPD

.  Tropicamide  [Mydriacyl]     Uses: Dilation of pupil

Adverse effects: Ocular Hypertension

.  Pirenzepine  [Gastrozepin]     Uses: Peptic Ulcers

.  Diphenhydramine  [Benadryl]      Uses: Antihistamine, sedative, hypnotic

.  Dimenhydrinate  [Dramamine]     Uses: Nausea, motion sickness

.  Dicycloverine      Uses: Irritable Bowel Syndrome

.  Flavoxate     Uses: Urinary Bladder Spasm

.  Oxybutynin  [Ditropan]   Uses: Urinary frequency, loss of bladder control

.  Tiotropium  [Spiriva]    Uses: COPD

.  Cyclopentolate  –  Eye drops      Uses: Pediatric Eye Examinations

.  Trihexyphenidyl  [Artane]      Uses: Parkinson’s disease, Extrapyramidal side effects

. Tolterodine  [Detrol]       Uses: Urinary Incontinence

.  Solifenacin [Vesicare]      Uses: Overactive Bladder

.  Darifenacin  [Enablex]      Uses: Urinary Incontinence, Overactive Bladder

.  Benzatropine  [Cogentin]    Uses: Parkinson’s Disease, Extrapyramidal side effects, Dystonia

. Mebeverine  [Colofac]      Uses: Irritable Bowel Syndrome, GI spasms

2.)  Antinicotinic Medications

Examples of Antinicotinic Medications

–  Method of action affects the “nicotinic acetylcholine receptors

–  These compounds are often used during surgery for paralysis while others can be used for drug addiction.

They can be divided into a few categories

1.)  Ganglionic Blocking Agents

2.)  Neuromuscular Blocking Agents [Non-depolarizing]

3.)  Neuromuscular Blocking Agents [Depolarizing]

4.)  Centrally Acting Nicotinic Antagonists

Ganglionic Blocking Agents

.  Mecamylamine        Uses: Previously used in Hypertension now primarily used as a research tool

.  Trimethaphan  [Arfonad]      Uses: Hypertensive Crisis, Dissecting Aortic Aneurysm, Pulmonary Edema, Bleeding during neurosurgery

Method of Action: Binds and blocks the sympathetic nervous system and parasympathetic nervous system.

Neuromuscular Blocking Agents [Non-depolarizing]

.  Atracurium      Uses: Anesthesia, Skeletal muscle relation

.  Doxacurium       Uses: Muscle relaxer

.  Mivacuriuim        Uses: Neuromuscular blocker or Muscle relaxant

.  Pancuronium       Uses: Muscle relaxant, General Anaesthesia – one of the drugs given during the “legal injection” in the United States.

In some European countries such as Belgium and Netherlands is used in the protocol for euthanasia

.  Tubocurarine     Uses: Anaesthesia         Used rarely

.  Vecuronium [Norcuron]     Uses: Muscle Relaxant

Neuromuscular Blocking Agents [Depolarizing]

.  Succinylcholine      Uses: Anesthesia, Emergency Medicine, Malignant Hypertension

Centrally Acting Nicotinic Antagonists

.  18-Methoxycoronaridine     Uses: Is still in the phase or research and hasn’t been tested on humans