Belladonna and Opium

Paddock Laboratories, LLC

BELLADONNA & OPIUMRECTAL SUPPOSITORIES

FULL PRESCRIBING INFORMATION: CONTENTS*

• BELLADONNA AND OPIUM DESCRIPTION
  • Belladonna (16.2 mg) and Opium (30 mg):
  • Belladonna (16.2 mg) and Opium (60 mg):
• CLINICAL PHARMACOLOGY
• BELLADONNA AND OPIUM INDICATIONS AND USAGE
• BELLADONNA AND OPIUM CONTRAINDICATIONS
• WARNINGS
• PRECAUTIONS
  • Pregnancy Category C
  • Nursing Mothers
• BELLADONNA AND OPIUM ADVERSE REACTIONS
• DRUG ABUSE AND DEPENDENCE
• OVERDOSAGE
• BELLADONNA AND OPIUM DOSAGE AND ADMINISTRATION
  • Adults:
• HOW SUPPLIED
• Caution:
• PRINCIPAL DISPLAY PANEL - 16.2 mg/30 mg Suppository Label
• PRINCIPAL DISPLAY PANEL - 16.2 mg/60 mg Suppository Label

FULL PRESCRIBING INFORMATION

CII

BELLADONNA AND OPIUM DESCRIPTION

Each belladonna and opium suppository contains (in a water-soluble base consisting of Polyethylene Glycol 400, 1450, 8000 and Polysorbate 60):

Belladonna (16.2 mg) and Opium (30 mg):

Powdered opium 30 mg (Warning: May be habit forming.) and powdered belladonna extract 16.2 mg.

Belladonna (16.2 mg) and Opium (60 mg):

Powdered opium 60 mg (Warning: May be habit forming.) and powdered belladonna extract 16.2 mg.

This drug falls into the pharmacological/therapeutic class of narcotic analgesic/antispasmotic agents.

The pharmacologically active principles present in the belladonna extract component of belladonna and opium suppositories are:

Established Name: Atropine Chemical Name: dl Tropyl Tropate

Established Name: Scopolamine Chemical Name: dl Scopolamine

Opium contains more than twenty alkaloids, the principle ones being morphine (10%), narcotine (6%), papaverine (1%) and codeine (0.5%). The major pharmacologically active principle of the powdered opium component of belladonna and opium suppositories, however, is:

Name: Morphine Chemical Name: 7, 8-Didehydro-4, 5-epoxy- 17-Methyl-morphinan-3, 6-diol

CLINICAL PHARMACOLOGY

Through its parasympatholytic action, atropine relaxes smooth muscle resulting from parasympathetic stimulation. It is the dl isomer of l-hyoscyamine and therefore exhibits the same clinical effects. It is, however, approximately one-half as active peripherally as lhyoscyamine, the latter being the major active plant alkaloid. The dl isomer atropine is formed during the process of isolation of the belladonna extract.¹

Morphine, the major active principle of powdered opium, is responsible for the action of powdered opium although the other alkaloids present also contribute to it. The sedative and analgesic action of morphine, the effect desired by inclusion in belladonna and opium suppositories of powdered opium, are thought to be due to the depressant effect on the cerebral cortex, hypothalamus and medullary centers. In large doses, the opiates and their analogs also exhibit synaptic conduction in the spinothalamic tracts, depress the function of the reticular formation, the lemniscus and the thalamic relays, and inhibit spinal synaptic reflexes: but these inhibitor actions should not be elicited with therapeutic doses of the drug. Moderate doses of powdered opium should not alter the electroencephalogram.

The action of morphine consists mainly of a descending depression of the central nervous system. It exerts its analgesic action by increasing the pain threshold or the magnitude of stimulus required to evoke pain and by dulling the sensibility or reaction to pain. In addition to its action in abolishing pain, morphine induces a sense of well-being (euphoria) facilitating certain mental processes while retarding others. Upon absorption of morphine, oxidative dealkylation to produce nor-compounds appears to be the first step in the reaction sequence which imparts analgesia. Morphine is conjugated in the liver to form the 3-glucuronide which passes into the bile and is reabsorbed and excreted in the urine. The atropine effect of the belladonna extract serves to eliminate morphine induced smooth muscle spasm without affecting the sedative analgesic action of powdered opium.²

BELLADONNA AND OPIUM INDICATIONS AND USAGE

Belladonna and opium suppositories are used for relief of moderate to severe pain associated with ureteral spasm not responsive to non-narcotic analgesics and to space intervals between injections of opiates.

BELLADONNA AND OPIUM CONTRAINDICATIONS

Do not use belladonna and opium suppositories in patients suffering from glaucoma, severe hepatic or renal disease, bronchial asthma, narcotic idiosyncrasies, respiratory depression, convulsive disorders, acute alcoholism, delirium tremens and premature labor.

WARNINGS

True addiction may result from opium usage. These preparations are not recommended for use in children.

PRECAUTIONS

Administer with caution to persons with a known idiosyncrasy to atropine or to atropinelike compounds; to persons known to be sensitive to or addicted to morphine or morphinelike drugs; to persons with cardiac disease, incipient glaucoma or prostatic hypertrophy. Caution should be used in the administration of this drug to elderly and debilitated patients and patients with increased intracranial pressure, toxic psychosis and myxedema.

Pregnancy Category C

Animal studies have not been conducted with belladonna and opium suppositories. It is also not known whether belladonna and opium suppositories can affect reproductive capacity. The active principles of belladonna and opium suppositories, atropine and morphine, are known to enter the fetal circulation. Regular use of opium alkaloids during pregnancy has resulted in addiction of the fetus leading to withdrawal symptoms in the neonate. Belladonna and opium suppositories therefore should be used by a pregnant woman with caution and only when clearly indicated.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when belladonna and opium suppositories are administered to a nursing woman.

BELLADONNA AND OPIUM ADVERSE REACTIONS

Belladonna may cause drowsiness, dry mouth, urinary retention, photophobia, rapid pulse, dizziness and blurred vision. Opium usage may result in constipation, nausea or vomiting. Pruritis and urticaria may occasionally occur.

DRUG ABUSE AND DEPENDENCE

Because of their content of opium, belladonna and opium suppositories are considered as Schedule II drugs by the Drug Enforcement Administration. No data exists on chronic abuse effects or dependence characteristics of belladonna and opium suppositories.

OVERDOSAGE

As with morphine and related narcotics, overdosage is characterized by respiratory depression, pinpoint pupils and coma. Respiratory depression may be reversed by intravenous administration of naloxone hydrochloride. In addition, supportive measures such as oxygenation, intravenous fluids and vasopressors should be used as indicated. As with atropine derivatives, hot, dry, flushed skin; dry mouth and hyperpyrexia may occur.

BELLADONNA AND OPIUM DOSAGE AND ADMINISTRATION

Adults:

One belladonna and opium suppository rectally once or twice daily, not to exceed four doses daily or as recommended by the physician. Moisten finger and suppository with water before inserting. Absorption is dependent on body hydration and not on body temperature.

Not recommended for use in children 12 years of age and under.

Store at room temperature. DO NOT REFRIGERATE. PROTECT FROM MOISTURE DURING STORAGE.

HOW SUPPLIED

Belladonna (16.2 mg) and Opium (30 mg) suppositories are easy to open, color-coded and available in cartons of 12's.

•  12's     NDC 0574-7045-12

Belladonna (16.2 mg) and Opium (60 mg) suppositories are easy to open, color coded and available in cartons of 12's.

•  12's     NDC 0574-7040-12

Schedule II controlled substances-DEA order required.

Caution:

Federal law prohibits transfer of this drug to any person other than the patient for whom it was prescribed.

1. Gilman, A.G., Goodman, L.S. & Gilman, A 6th Edition, The Pharmacological Basis of Therapeutics, MacMillan Pub. Co., NY 1980, pp. 121-127

2. Ibid, pp. 494-513

Manufactured by:
Paddock Laboratories, Inc.
Minneapolis, MN 55427

(07-05)

PRINCIPAL DISPLAY PANEL - 16.2 mg/30 mg Suppository Label

BELLADONNA AND OPIUM
16.2 mg/30 mg Suppository
(01)10305747045121

CII

Paddock Laboratories, Inc.
Minneapolis, MN 55427

PRINCIPAL DISPLAY PANEL - 16.2 mg/60 mg Suppository Label

Belladonna & Opium
16.2 mg/60 mg Suppository
(01)10305747040126

CII

Paddock Laboratories, Inc.
Minneapolis, MN 55427