Atropine/diphenoxylate

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Atropine/diphenoxylate
Combination of
Diphenoxylate Mu opiate receptor agonist
Atropine Muscarinic acetylcholine receptors antagonist
Clinical data
Trade names Lomotil
AHFS/Drugs.com Professional Drug Facts
License data
Pregnancy
category
  • AU:C
Routes of
administration 		By mouth
ATC code
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Legal status
Legal status
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CAS Number
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Diphenoxylate/atropine, also known as co-phenotrope, is a combination of the medications diphenoxylate and atropine, used to treat diarrhea. [2] [3] It should not be used in those in whom Clostridioides difficile infection is a concern. [4] It is taken by mouth. [2] Onset is typically within an hour. [5]

Contents

Side effects may include abdominal pain, angioedema, glaucoma, heart problems, feeling tired, dry mouth, and trouble seeing. [2] It is unclear if use in pregnancy is safe and use when breastfeeding may result in side effects in the baby. [6] It works by decreasing contractions of the bowel. [2]

The combination was approved for medical use in the United States in 1960. [5] It is available as a generic medication. [2] In 2021, it was the 293rd most commonly prescribed medication in the United States, with more than 600,000 prescriptions. [7] [8] It is sold under the brand name Lomotil among others. [2] The medication is in Schedule V in the United States. [4]

Contraindications

Absolute contraindications are: [9] [10]

Side effects


The drug combination is generally safe for short-term use and with recommended dosage. In doses used for the treatment of diarrhea, whether acute or chronic, diphenoxylate has not produced addiction.

It may cause several side-effects, such as dry mouth, headache, constipation and blurred vision. Since it may also cause drowsiness or dizziness, it should not be used by motorists, operators of hazardous machinery, etc. It is not recommended for children under two years of age.

Interactions

Interactions with other drugs:

Diarrhea that is caused by some antibiotics such as cefaclor, erythromycin or tetracycline can worsen. [12]

Toxicity

It may cause serious health problems when overdosed. Signs and symptoms of adverse effects may include any or several of the following: convulsions, respiratory depression (slow or stopped breathing), dilated eye pupils, nystagmus (rapid side-to-side eye movements), erythema (flushed skin), gastrointestinal constipation, nausea, vomiting, paralytic ileus, tachycardia (rapid pulse), drowsiness and hallucinations. Symptoms of toxicity may take up to 12 hours to appear.

Treatment of overdose must be initiated immediately after diagnosis and may include the following: ingestion of activated charcoal, laxative and a counteracting medication (narcotic antagonist). [12]

Mechanism of action

Diphenoxylate is anti-diarrheal and atropine is anticholinergic. A subtherapeutic amount of atropine sulfate is present to discourage deliberate overdosage. Atropine has no anti-diarrheal properties, but will cause tachycardia when overused. The medication diphenoxylate works by slowing down the movement of the intestines. In some cases it has been shown to ease symptoms of opiate withdrawal.

History

Diphenoxylate was developed in 1954 as part of US Navy and CIA-funded research on nonaddictive substitutes for codeine. [13]

Society and culture

Names

The UK British Approved Name (BAN) generic name for diphenoxylate and atropine is co-phenotrope.[ citation needed ]

As of 2018, the combination drug is marketed in the US and some other countries under the following brands: Atridol, Atrolate, Atrotil, Co-Phenotrope, Dhamotil, Dimotil, Intard, Logen, Lomanate, Lomotil, Lonox, and Reasec. [14]

In the United States, it is classified as a Schedule V controlled substance by federal law, and is available only for a medical purpose. [15]

Related Research Articles

<span class="mw-page-title-main">Diarrhea</span> Loose or liquid bowel movements

Diarrhea, also spelled diarrhoea or diarrhœa, is the condition of having at least three loose, liquid, or watery bowel movements in a day. It often lasts for a few days and can result in dehydration due to fluid loss. Signs of dehydration often begin with loss of the normal stretchiness of the skin and irritable behaviour. This can progress to decreased urination, loss of skin color, a fast heart rate, and a decrease in responsiveness as it becomes more severe. Loose but non-watery stools in babies who are exclusively breastfed, however, are normal.

<span class="mw-page-title-main">Atropine</span> Anticholinergic medication used as antidote for nerve agent poisoning

Atropine is a tropane alkaloid and anticholinergic medication used to treat certain types of nerve agent and pesticide poisonings as well as some types of slow heart rate, and to decrease saliva production during surgery. It is typically given intravenously or by injection into a muscle. Eye drops are also available which are used to treat uveitis and early amblyopia. The intravenous solution usually begins working within a minute and lasts half an hour to an hour. Large doses may be required to treat some poisonings.

<span class="mw-page-title-main">Benzatropine</span> Medication for movement disorders

Benzatropine (INN), known as benztropine in the United States and Japan, is a medication used to treat movement disorders like parkinsonism and dystonia, as well as extrapyramidal side effects of antipsychotics, including akathisia. It is not useful for tardive dyskinesia. It is taken by mouth or by injection into a vein or muscle. Benefits are seen within two hours and last for up to ten hours.

<span class="mw-page-title-main">Hyoscyamine</span> Tropane alkaloid

Hyoscyamine is a naturally occurring tropane alkaloid and plant toxin. It is a secondary metabolite found in certain plants of the family Solanaceae, including henbane, mandrake, angel's trumpets, jimsonweed, the sorcerers' tree, and Atropa belladonna. It is the levorotary isomer of atropine and thus sometimes known as levo-atropine.

<span class="mw-page-title-main">Loperamide</span> Medicine used to reduce diarrhea

Loperamide, sold under the brand name Imodium, among others, is a medication of the opioid receptor agonist class used to decrease the frequency of diarrhea. It is often used for this purpose in irritable bowel syndrome, inflammatory bowel disease, short bowel syndrome Crohn's disease and ulcerative colitis. It is not recommended for those with blood in the stool, mucus in the stool, or fevers. The medication is taken by mouth.

Anticholinergics are substances that block the action of the acetylcholine (ACh) neurotransmitter at synapses in the central and peripheral nervous system.

<span class="mw-page-title-main">Dicycloverine</span> Antispasmodic agent

Dicycloverine, also known as dicyclomine, sold under the brand name Bentyl among others, is a medication that is used to treat spasms of the intestines such as those that occur in irritable bowel syndrome. It is taken by mouth or by injection into a muscle. While it has been used in baby colic and enterocolitis, evidence does not support these uses.

<span class="mw-page-title-main">Ipratropium bromide</span> Type of anticholinergic

Ipratropium bromide, sold under the trade name Atrovent among others, is a type of anticholinergic medication which is applied by different routes: inhaler, nebulizer, or nasal spray, for different reasons.

<span class="mw-page-title-main">Lansoprazole</span> Stomach acid suppressing medication

Lansoprazole, sold under the brand name Prevacid among others, is a medication which reduces stomach acid. It is a proton pump inhibitor (PPI), used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. Its effectiveness is similar to that of other PPIs. It is taken by mouth. Onset is over a few hours and effects last up to a couple of days.

<span class="mw-page-title-main">Diphenoxylate</span> Centrally active opioid drug used for the treatment of diarrhea

Diphenoxylate is a centrally active opioid drug of the phenylpiperidine series that is used as a combination drug with atropine for the treatment of diarrhea. Diphenoxylate is an opioid and acts by slowing intestinal contractions; the atropine is present to prevent drug abuse and overdose. It should not be given to children due to the risk that they will stop breathing and should not be used in people with Clostridioides difficile infection.

<span class="mw-page-title-main">Tolterodine</span> Benzhydryl compound

Tolterodine, sold under the brand name Detrol among others, is a medication used to treat frequent urination, urinary incontinence, or urinary urgency. Effects are seen within an hour. It is taken by mouth.

<span class="mw-page-title-main">Levocetirizine</span> Antihistamine drug

Levocetirizine, sold under the brand name Xyzal, among others, is a second-generation antihistamine used for the treatment of allergic rhinitis and long-term hives of unclear cause. It is less sedating than older antihistamines. It is taken by mouth.

<span class="mw-page-title-main">Isoprenaline</span> Medication for slow heart rate

Isoprenaline, also known as isoproterenol and sold under the brand name Isuprel among others, is a sympathomimetic medication which is used in the treatment of acute bradycardia, heart block, and rarely for asthma, among other indications. It is used by injection into a vein, muscle, fat, or the heart, by inhalation, and in the past under the tongue or into the rectum.

<span class="mw-page-title-main">Tizanidine</span> Muscle relaxant medication

Tizanidine, sold under the brand name Zanaflex among others, is an alpha-2 (α2) adrenergic receptor agonist, similar to clonidine, that is used to treat muscle spasticity due to spinal cord injury, multiple sclerosis, and spastic cerebral palsy. Effectiveness appears similar to baclofen or diazepam. It is taken by mouth.

<span class="mw-page-title-main">Biperiden</span> Group of stereoisomers

Biperiden, sold under the brand name Akineton among others, is a medication used to treat Parkinson disease, certain drug-induced movement disorders and Tourette Syndrome. It is not recommended for tardive dyskinesias. It is taken by mouth, injection into a vein, or muscle.

<span class="mw-page-title-main">Cefdinir</span> Chemical compound

Cefdinir, sold under the brand name Omnicef among others, is an antibiotic used to treat pneumonia, otitis media, strep throat, and cellulitis. It is a less preferred option for pneumonia, otitis media, and strep throat which may be used in those with a severe allergy to penicillin. It is taken by mouth.

Motofen is the brand name for an antiperistaltic anti-diarrheal medication, containing 1.0 mg difenoxin HCl and 0.025 mg atropine. It was invented by Kendra Clark. Atropine is purposely added at 25 micrograms per tablet, or 1/24 to 1/40 of the usual therapeutic dose for atropine to minimize the potential of misuse by swallowing large numbers of tablets or preparing them for injection since difenoxin is chemically related to the pethidine-piritramide subgroup of the opioid family, and could theoretically be misused. Although unlikely, physical and mental withdrawal symptoms are possible if taken for long periods of time. However, both of these compounds are responsible for the medicinal effects of the medicine.

<span class="mw-page-title-main">Difenoxin</span> Chemical compound

Difenoxin is an opioid drug used, often in combination with atropine, to treat diarrhea. It is the principal metabolite of diphenoxylate.

Losartan/hydrochlorothiazide, sold under the brand name Hyzaar among others, is a fixed-dose combination medication used to treat high blood pressure when losartan is not sufficient. It consists of losartan, an angiotensin II receptor blocker; and hydrochlorothiazide, a thiazide diuretic. It is taken by mouth.

Antimotility agents are drugs used to alleviate the symptoms of diarrhea. These include loperamide (Imodium), bismuth subsalicylate (Pepto-Bismol), diphenoxylate with atropine (Lomotil), and opiates such as paregoric, tincture of opium, codeine, and morphine. In diarrhea caused by invasive pathogens such as Salmonella, Shigella, and Campylobacter, the use of such agents has generally been strongly discouraged, though evidence is lacking that they are harmful when administered in combination with antibiotics in Clostridioides difficile cases. Use of antimotility agents in children and the elderly has also been discouraged in treatment of EHEC due to an increased rate of hemolytic uremic syndrome.

References

  1. ↑ "Lomotil- diphenoxylate hydrochloride and atropine sulfate tablet". DailyMed. U.S. National Library of Medicine. 25 October 2021. Retrieved 20 February 2022.
  2. 1 2 3 4 5 6 British National Formulary (76th ed.). Pharmaceutical Press. 2018. p. 66. ISBN   9780857113382.
  3. ↑ Jain M, Wylie WP (June 2021). "Diphenoxylate and Atropine". StatPerls. Treasure Island (FL): StatPearls Publishing. PMID   32644726.
  4. 1 2 "Diphenoxylate hydrochloride and atropine sulfate solution". DailyMed. U.S. National Library of Medicine. Retrieved 22 March 2019.
  5. 1 2 "Diphenoxylate and Atropine (Professional Patient Advice)". Drugs.com. Retrieved 22 March 2019.
  6. ↑ "Atropine / diphenoxylate Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  7. ↑ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  8. ↑ "Atropine; Diphenoxylate - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  9. ↑ Rio V (15 August 2019). "Lomotil (diphenoxylate/atropine)". Medical News Today. Archived from the original on 28 September 2020.
  10. ↑ "Lomotil". RxList. Archived from the original on 28 October 2008.
  11. 1 2 3 "Diphenoxylate and atropine drug information" . UpToDate. Retrieved 14 February 2017.
  12. 1 2 Jain M, Wylie WP (2023). "Diphenoxylate and Atropine". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID   32644726 . Retrieved 23 June 2023.
  13. ↑ "Memorandum for the Secretary of Defense" (PDF). Archived (PDF) from the original on 16 September 2017. Retrieved 28 July 2013.
  14. ↑ "Diphenoxylate international brands". Drugs.com. Retrieved 11 May 2018.
  15. ↑ DEA, Title 21, Section 829
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