Atrolate

Atrolate Uses, Dosage, Side Effects, Food Interaction and all others data.

Atropine binds to and inhibit muscarinic acetylcholine receptors, producing a wide range of anticholinergic effects. Atropine is an anticholinergic agent which competitively blocks the muscarinic receptors in peripheral tissues such as the heart, intestines, bronchial muscles, iris and secretory glands. Some central stimulation may occur. Atropine abolishes bradycardia and reduces heart block due to vagal activity. Smooth muscles in the bronchi and gut are relaxed while glandular secretions are reduced. It also has mydriatic and cycloplegic effect.

Atropine, a naturally occurring belladonna alkaloid, is a racemic mixture of equal parts of d- and l-hyoscyamine, whose activity is due almost entirely to the levo isomer of the drug. Atropine is commonly classified as an anticholinergic or antiparasympathetic (parasympatholytic) drug. More precisely, however, it is termed an antimuscarinic agent since it antagonizes the muscarine-like actions of acetylcholine and other choline esters. Adequate doses of atropine abolish various types of reflex vagal cardiac slowing or asystole. The drug also prevents or abolishes bradycardia or asystole produced by injection of choline esters, anticholinesterase agents or other parasympathomimetic drugs, and cardiac arrest produced by stimulation of the vagus. Atropine may also lessen the degree of partial heart block when vagal activity is an etiologic factor. Atropine in clinical doses counteracts the peripheral dilatation and abrupt decrease in blood pressure produced by choline esters. However, when given by itself, atropine does not exert a striking or uniform effect on blood vessels or blood pressure.

A meperidine congener used as an antidiarrheal, usually in combination with atropine. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. This medication is classified as a Schedule V under the Controlled Substances Act by the Food and Drug Administration (FDA) and the DEA in the United States when used in preparations. When diphenoxylate is used alone, it is classified as a Schedule II.

Diphenoxylate, an antidiarrheal, is effective as adjunctive therapy in the management of diarrhea. Diphenoxylate is rapidly and extensively metabolized in man by ester hydrolysis to diphenoxylic acid (difenoxine), which is biologically active and the major metabolite in the blood.

Atrolate
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Atrolate
Generic	Atropine + Diphenoxylate
Weight	25mcg, 2.5mg
Type	Tablet
Therapeutic Class
Manufacturer	Rex Pharmaceuticals Pakistan
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Atropine is used for Non ulcer dyspepsia, Irritable bowel syndrome, Diverticular disease, Bradycardia, Organophosphorus poisoning, Premedication in anesthesia, Poisoning or overdosage with compound having muscarinic actions, Ophthalmic Inflammatory eye disorders, Eye refraction.

Diphenoxylate is an antidiarrheal medication used with atropine to manage diarrhea.

For as adjunctive therapy in the management of diarrhea

Atrolate is also used to associated treatment for these conditions: Amblyopia, Atrioventricular Heart Block, Bradycardia, Bronchospasm, Crying, Detrusor Hyperreflexia, Excessive bronchial secretion, Hypertonic uterine contraction, Hypertonicity of the small intestine, Ocular Inflammation, Parkinsonism, Peptic Ulcer, Poisoning by parasympathomimetics (cholinergics), Poisoning caused by mushrooms, Poisoning caused by organophosphate anticholinesterase nerve agents, Poisoning caused by organophosphorus pesticides, Pylorospasm, Rhinorrhoea, Sinus Bradycardia, Spasms, Toxic effect of organophosphate and carbamate, Hypermobility of the colon, Laughing, Muscarinic side effectsDiarrhoea

How Atrolate works

Atropine binds to and inhibit muscarinic acetylcholine receptors, producing a wide range of anticholinergic effects.

Diphenoxylate is an opiate receptor agonists that stimulate mu receptors in GI to decrease the peristalsis and constrict the sphincters. Diphenoxylate has a direct effect on circular smooth muscle of the bowel, that conceivably results in segmentation and prolongation of gastrointestinal transit time. The clinical antidiarrheal action of diphenoxylate may thus be a consequence of enhanced segmentation that allows increased contact of the intraluminal contents with the intestinal mucosa.

Dosage

Atrolate dosage

Adult:

IV: Bradycardia: 500 mcg every 3-5 mins. Total: 3 mg.
IV/IM: Organophosphorus poisoning: 2 mg every 10-30 mins until muscarinic effects disappear or atropine toxicity appears.
IM/SC: Premedication in anesthesia: 300-600 mcg 30-60 mins before anesthesia.
IV/IM/SC: Poisoning or overdosage with compound having muscarinic actions: 0.6-1 mg, repeat 2 hrly.
Ophthalmic: Inflammatory eye disorders: As 0.5-1% solution: 1-2 drops 4 times/day.
Ophthalmic: refraction: 1% solution 1 drop twice daily for 1-2 days before procedure.
Oral: Non ulcer dyspepsia, Irritable bowel syndrome, Diverticular disease: 0.6-1.2 mg as a single dose at bedtime.

Usual Pediatric Dose for Anesthesia:

7 to 16 pounds: 0.1 mg, IV, IM, or subcutaneously
17 to 24 pounds: 0.15 mg, IV, IM, or subcutaneously
24 to 40 pounds: 0.2 mg, IV, IM, or subcutaneously
40 to 65 pounds: 0.3 mg, IV, IM, or subcutaneously
65 to 90 pounds: 0.4 mg, IV, IM, or subcutaneously
Over 90 pounds: 0.4 to 0.6 mg, IV, IM, or subcutaneously

Side Effects

Injection: Dry mouth, dysphagia, constipation, flushing and dryness of skin, tachycardia, palpitations, arrhythmias, mydriasis, photophobia, cycloplegia, raised intraocular pressure. Toxic doses cause tachycardia, hyperpyrexia, restlessness, confusion, excitement, hallucinations, delirium and may progress to circulatory failure and resp depression.

Eye drops or ointment: Systemic toxicity esp in children, on prolonged use may lead to irritation, hyperaemia, oedema and conjunctivitis. Increased intraocular pressure.

Toxicity

Oral, mouse: LD₅₀ = 75 mg/kg. Symptoms of overdose includes widespread paralysis of parasympathetically innervated organs. Dry mucous membranes, widely dilated and nonresponsive pupils, tachycardia, fever and cutaneous flush are especially prominent, as are mental and neurological symptoms. In instances of severe intoxication, respiratory depression, coma, circulatory collapse and death may occur.

Coma, dry skin and mucous membranes, enlarged pupils of the eyes, extremely high body temperature, flushing, involuntary eyeball movement, lower than normal muscle tone, pinpoint pupils, rapid heartbeat, restlessness, sluggishness, suppressed breathing

Precaution

Reflux oesophagitis; elderly; infants and children; Pregnancy.

Interaction

Additive anticholinergic effects with quinidine, antidepressants and some antihistamines.

Elimination Route

Atropine is rapidly and well absorbed after intramuscular administration. Atropine disappears rapidly from the blood and is distributed throughout the various body tissues and fluids.

90%

Half Life

3.0 ± 0.9 hours in adults. The half-life of atropine is slightly shorter (approximately 20 minutes) in females than males.

12-14 hours

Elimination Route

Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver; from 13 to 50% is excreted unchanged in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category C. Animal reproduction studies have not been conducted with atropine. It also is not known whether atropine can cause fetal harm when given to a pregnant woman or can affect reproduction capacity. Atropine should be given to a pregnant woman only if clearly needed.

Contraindication

Glaucoma, chronic respiratory disease, sick sinus syndrome, thyrotoxicosis, cardiac failure, pyloric stenosis, prostatic hypertrophy.

Acute Overdose

May cause hyperthermia, hypertension, increased respiratory rate, nausea and vomiting. May also lead to CNS stimulation. Severe intoxication may lead to CNS depression, coma, respiratory failure and death.