diphenoxylate/atropine (Rx)

Brand and Other Names:Lomotil
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

diphenoxylate HCl/atropine (Schedule V)

tablet

  • 2.5mg/0.025mg

solution

  • 2.5mg/0.025mg/5mL
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Diarrhea

5 mg diphenoxylate/0.05 mg atropine (2 tablets) PO q6hr; not to exceed 20 mg diphenoxylate daily until initial control of diarrhea achieved (ususally 48 hr)

Contact physician is diarrhea continues beyond 48 hr

Maintenance: As low as ¼ of initial dosage

Dosage Forms & Strengths

diphenoxylate HCl/atropine (Schedule V)

tablet

  • 2.5mg/0.025mg

solution

  • 2.5mg/0.025mg/5mL
more...

Diarrhea

<13 years: Safety and efficacy not established

≥13 years: 5 mg diphenoxylate/0.05 mg atropine PO q6hr; not to exceed 20 mg diphenoxylate daily until initial control of diarrhea achieved (ususally 48 hr)

Contact physician is diarrhea continues beyond 48 hr

Maintenance: As low as ¼ of initial dosage

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Interactions

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            Adverse Effects

            1-10%

            Anticholinergic effects

            Blurred vision

            Sedation

            Nausea

            Vomiting

            Abdominal discomfort

            Dryness of skin or mouth

            Frequency Not Defined

            Pancreatitis

            Toxic megacolon

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            Warnings

            Contraindications

            Hypersensitivity to diphenoxylate or atropine

            Children aged <6 years owing to risks of respiratory and CNS depression

            Obstructive jaundice

            Diarrhea associated with pseudomembranous enterocolitis or infectious enterotoxin-producing bacteria

            Cautions

            Cases of severe respiratory depression and coma, leading to permanent brain damage or death reported in children aged <6 years (see Contraindications)

            Use should be accompanied by appropriate fluid and electrolyte therapy, when indicated; if severe dehydration or electrolyte imbalance present, drug should be withheld until appropriate corrective therapy initiated; drug-induced inhibition of peristalsis may result in fluid retention in intestine, which may further aggravate dehydration and electrolyte imbalance

            Use with extreme caution in patients with advanced hepatorenal disease and in all patients with abnormal liver function; hepatic coma may be precipitated

            In patients with acute ulcerative colitis, agents that inhibit intestinal motility or prolong intestinal transit time reported to induce toxic megacolon; patients with acute ulcerative colitis should be carefully observed and therapy discontinued promptly if abdominal distention occurs or if other untoward symptoms develop

            Improvement of symptoms expected within 48 hours; if no improvement within this time, drug is unlikely to be effective

            Do not exceed recommended dosage; reduce initial dosage for maintenance

            Give consideration to development of adverse reactions associated with of atropine; therapy has caused atropinism (hyperthermia, tachycardia, urinary retention, flushing, dryness of the skin and mucous membranes) particularly in pediatric patients with Down’s syndrome; therapy is not indicated for use in pediatric patients monitor patients for signs of atropinism

            Diphenoxylate hydrochloride may potentiate action of other drugs that cause dizziness or drowsiness, including barbiturates, benzodiazepines and other sedatives/hypnotics, anxiolytics, and tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, and alcohol; patient should be closely observed when any of these are used concomitantly

            Renal impairment

            Hepatic impairment

            Coadministration with opioids increases risk of anticholinergic and opioid toxicities; initial presenting symptoms may be delayed by up to 30 hr due to prolonged gastric emptying time induced by diphenoxylate

            Therapy contraindicated in patients with diarrhea associated with organisms that penetrate the GI mucosa; antiperistaltic agents, slow gastrointestinal motility and may enhance bacterial overgrowth and release of bacterial exotoxins; drug has been reported to result in serious GI complications in patients with infectious diarrhea, including sepsis, prolonged and/or worsened diarrhea; prolonged fever and the delay in resolution of stool pathogens reported in study of Shigellosis in adults

            Since chemical structure of diphenoxylate hydrochloride is similar to that of meperidine hydrochloride, concurrent use with monoamine oxidase (MAO) inhibitors may, in theory, precipitate hypertensive crisis

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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies in pregnant women; drug should be used during pregnancy only if anticipated benefit justifies potential risk to fetus; diphenoxylate hydrochloride shown to have effect on fertility in rats when given in doses 50 times human dose; a decrease in maternal weight gain of 30% at 20 mg/kg/day and of 10% at 4 mg/kg/day; at 10 times human dose (4 mg/kg/day), average litter size was slightly reduced

            Lactation

            Exercise caution when drug is administered to nursing woman, since physicochemical characteristics of major metabolite, diphenoxylic acid, are such that it may be excreted in breast milk and since it is known that atropine is excreted in breast milk

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Diphenoxylate: Acts on smooth muscle of intestinal tract, inhibiting GI motility and excessive GI propulsion (like morphine)

            Atropine: Subtherapeutic quantity of atropine is added to discourage deliberate overdose of diphenoxylate

            Absorption

            Onset: 45 min-1 hr 

            Duration: 3-4 hr 

            Peak plasma time: 2 hr 

            Bioavailability: 90% 

            Distribution

            Vd: 324.2 L

            Metabolism

            Extensively metabolized in liver to active metabolite, diphenoxylic acid (difenoxin), which is 5 times more potent than diphenoxylate 

            Metabolites: Diphenoxylic acid (active), hydroxydiphenoxylic acid (inactive)

            Elimination

            Half-life: 2.5 hr (diphenoxylate); 3-14 hr (diphenoxylic acid)

            Renal clearance: 1483 mL/min 

            Excretion: Feces via bile (49%), urine (14%) 

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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