AHFS Class:
- Antidiarrhea Agents 56:08
Generic Name(s):
Opium, a naturally occurring opiate agonist, is an antiperistaltic antidiarrhea agent.
Opium preparations are used for their constipating effect in the symptomatic treatment of diarrhea. Although paregoric is widely used, the less complex and more potent opium tincture is preferred by some clinicians. Opium preparations should not be used in patients with diarrhea caused by poisoning until the toxic material is eliminated from the GI tract by gastric lavage or cathartics. Opium preparations are frequently used in combination with kaolin and pectin, which have adsorbent and protective properties. Bismuth salts are also common ingredients in commercially available opium preparation combination products, presumably for their adsorbent and protective effects.
Paregoric and diluted opium tincture also have been used to manage manifestations of opiate abstinence syndrome (i.e., postnatal withdrawal) in neonates† exposed to opiates in utero.350,351,352,353,355,357 However, because of the alcohol content of these preparations, the potential for medication errors resulting from confusion of opium tincture (i.e., deodorized opium tincture) and diluted opium tincture, and the potential for adverse effects from excipients contained in paregoric, other opiates currently are preferred for the management of neonatal opiate abstinence syndrome when environmental and supportive measures are inadequate and pharmacologic therapy is required.350,351,352,353,355,357 (See Uses: Neonatal Opiate Withdrawal, in the Opiate Agonists General Statement 28:08.08.)
Administration 
Paregoric and opium tincture are administered orally. When paregoric is added to water, a milky fluid is formed by the separation of anise oil and camphor.
Dosage
The usual adult dosage of paregoric for the treatment of diarrhea is 5-10 mL 1-4 times daily. The usual pediatric dosage of paregoric is 0.25-0.5 mL/kg 1-4 times daily.
The usual adult dosage of opium tincture for the treatment of diarrhea is 0.6 mL 4 times daily and may range from 0.3-1 mL 4 times daily. Single doses should not exceed 1 mL and dosage should not exceed 6 mL daily. Opium tincture contains 25 times more morphine than does paregoric and should never be confused with the latter preparation.
Nausea and other GI disturbances may occur occasionally in patients receiving opium preparations for the treatment of diarrhea. In usual oral antidiarrheal doses, opium does not produce analgesia or euphoria; therefore, opium preparations may be used in the treatment of acute diarrhea with little risk of development of physical dependence in the patient. Prolonged use of opium preparations, however, as in patients with ileitis or colitis, may produce physical dependence.
Opium preparations should be used with caution in patients with asthma, severe prostatic hypertrophy, hepatic disease, or with a history of opiate agonist dependence.
Acute Toxicity
Acute toxicity of opium preparations is manifested by depression of the CNS and may be reversed by administration of an opiate antagonist (i.e., naloxone hydrochloride).
Pharmacology
Opium, because of its morphine content, increases smooth muscle tone of the GI tract, inhibits GI motility and propulsion, and diminishes digestive secretions. Normal peristaltic movements are thus inhibited and the passage of intestinal contents is delayed; the feces become desiccated and constipation results. Relatively small doses of opium that are effective in controlling diarrhea do not produce substantial analgesia. The papaverine content of the mixed alkaloids is too small to have demonstrable smooth muscle relaxant activity.
Pharmacokinetics
Absorption
Following oral administration, morphine is variably absorbed from the GI tract. The drug is rapidly metabolized following oral administration, however, and plasma concentrations of unconjugated morphine are lower than those achieved after parenteral administration.
Elimination
Opium preparations are metabolized in the liver. Morphine undergoes conjugation with glucuronic acid at the 3-hydroxyl group. Secondary conjugation may also occur at the 6-hydroxyl group to form the 3,6-diglucuronide. Morphine is excreted in the urine mainly as morphine-3-glucuronide and smaller amounts of morphine-3,6-diglucuronide and unchanged drug. Approximately 75% of a dose of morphine is excreted in urine within 48 hours.
Chemistry and Stability
Chemistry
Opium is the air-dried milky exudate obtained by incising the unripe capsules of Papaver somniferum Linné or its variety album De Candolle. Opium contains several alkaloids, including not less than 9.5% anhydrous morphine and small amounts of codeine and papaverine. Powdered opium is opium dried at a temperature not exceeding 70°C and reduced to a very fine powder. Powdered opium (no longer commercially available in the US) contains 10-10.5% anhydrous morphine and may have inert, nontoxic diluents (except starch) added. Powdered opium occurs as a light brown or moderately yellowish-brown powder. Paregoric contains 2 mg of anhydrous morphine (usually as powdered opium, or as opium or opium tincture), 0.02 mL of anise oil, 20 mg of benzoic acid, 20 mg of camphor, 0.2 mL of glycerin, and sufficient diluted alcohol to make 5 mL. Opium tincture is an alcoholic solution containing 50 mg of anhydrous morphine (as granulated or sliced opium) per 5 mL.
Stability
Paregoric and opium tincture should be stored in tight, light-resistant containers; exposure to direct sunlight and to excessive heat should be avoided.
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Opium preparations are subject to control under the Federal Controlled Substances Act of 1970 as schedule II (C-II) drugs, but as schedule III (C-III) drugs when they contain 25 mg or less of opium per 5 mL, 5 g, or dosage unit in fixed combination with a therapeutic amount of one or more non-opiate drugs or as schedule V (C-V) drugs when they contain 1 mg or less of opium per mL or g in combination with one or more active non-opiate medicinal ingredients in sufficient proportion to confer on the preparation medicinal qualities not possessed by opium.
Opium Tincture (Deodorized Opium Tincture, Laudanum)
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|
Oral | Tincture | 50 mg (of morphine anhydrous) per 5 mL* | Opium Tincture Deodorized ( C-II ) | Marathon |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Paregoric (Camphorated Opium Tincture)
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|
Oral | Tincture | 2 mg (of morphine anhydrous) per 5 mL* | Paregoric ( C-III ) | |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
AHFS® Drug Information. © Copyright, 1959-2024, Selected Revisions October 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Only references cited for selected revisions after 1984 are available electronically.
350. Substance Abuse and Mental Health Services Administration (SAMHSA) Clinical guidance for treating pregnant and parenting women with opioid use disorder and their infants (HHS publication no. [SMA] 18-5054). Rockville, MD: SAMHSA. 2018. From SAMHSA website. [Web]
351. Klaman SL, Isaacs K, Leopold A et al. Treating Women Who Are Pregnant and Parenting for Opioid Use Disorder and the Concurrent Care of Their Infants and Children: Literature Review to Support National Guidance. J Addict Med . 2017 May/Jun; 11:178-190. [PubMed 28406856]
352. McQueen K, Murphy-Oikonen J. Neonatal Abstinence Syndrome. N Engl J Med . 2016; 375:2468-2479. [PubMed 28002715]
353. Hudak ML, Tan RC, COMMITTEE ON DRUGS et al. Neonatal drug withdrawal. Pediatrics . 2012; 129:e540-60. [PubMed 22291123]
355. Raffaeli G, Cavallaro G, Allegaert K et al. Neonatal Abstinence Syndrome: Update on Diagnostic and Therapeutic Strategies. Pharmacotherapy . 2017; 37:814-823. [PubMed 28519244]
357. Kocherlakota P. Neonatal abstinence syndrome. Pediatrics . 2014; 134:e547-61. [PubMed 25070299]