exoLERITINE® Injection LERITINE® Tablets
Action And Clinical Pharmacology: Anileridine, a synthetic opioid, is a strong analgesic. The chief pharmacologic action is exerted on the CNS. The analgesic effects usually are prompt in onset either orally or parenterally (approximately within 15 minutes). Duration of action is about 2 or 3 hours.
Respiratory depression, when it occurs, is of shorter duration than that seen with morphine or meperidine when equipotent analgesic doses are used.
Anileridine is absorbed by all routes of administration and is metabolized chiefly in the liver. Very little is excreted in the urine.
Indications And Clinical Uses: For the relief of moderate to severe pain (e.g., angina pectoris, renal colic, biliary colic, and pain associated with extensive burns, fractures, and carcinoma). In acute congestive heart failure for rest and relief of apprehension. In oral surgery for relief of pain including that of exodontia.
Anileridine also is useful in support of anesthesia and postoperatively. Satisfactory preoperative use has been reported.
Anileridine provides good obstetric analgesia alone and with both scopolamine and barbiturates. With the use of this analgesic, patients frequently relax and sleep between labor pains. Thus some degree of amnesia may be obtained.
Contra-Indications: The presence of respiratory depression; should be used with great caution, if at all, when respiratory failure is a possibility, as in head injury or brain tumor. Known hypersensitivity to the drug or any of the nonmedicinal ingredients of the preparations. Anileridine should not be used in patients 12 years of age and under because clinical experience in this age group is limited.
Manufacturers’ Warnings In Clinical States: As with morphine and meperidine, the possibility of addiction to anileridine should be kept in mind. The addiction potential of anileridine is regarded as being equal to that of morphine, inasmuch as anileridine will suppress completely the withdrawal symptoms of morphine addiction. Anileridine should not be given unnecessarily nor should its use be prolonged unduly.
As with other opioid analgesics, anileridine should be used with extreme caution in cases of severe hepatic insufficiency, severe CNS depression or coma, or in patients with head injuries and conditions in which intracranial pressure is increased, myxedema, Addison’s Disease, acute alcoholism, delirium tremens, convulsive disorders, and in patients taking MAO inhibitors.
Pregnancy: Safe use in pregnancy has not been established with regard to the possibility of adverse effects upon fetal development. Therefore, anileridine should be used in patients who are pregnant or in women of child bearing age only when the potential benefits outweigh the possible hazards.
The sudden i.v. injection of a dose greater than 10 mg may result in severe respiratory depression and/or apnea, hypotension and cardiac arrest. Therefore, anileridine should not be given by direct i.v. injection, except in extreme emergencies when time or lack of facilities will not permit the use of a diluted preparation (5 to 10 mg/10 mL saline 0.9%).
Precautions: Respiratory depression and, to a lesser degree, circulatory depression are the chief hazards attending the use of this analgesic. Respiratory depression occurs most frequently in the elderly, and debilitated patients and in those suffering from conditions accompanied by hypoxia or hypercapnia when even moderate therapeutic doses may dangerously decrease pulmonary ventilation. Anileridine should be given very cautiously to patients in shock, since the depressant effect upon respiration may act indirectly to further reduce the circulating blood volume, cardiac output, and blood pressure.
If deep respiratory depression and circulatory collapse appear to be imminent in those patients after the administration of anileridine, the administration of naloxone may assist in counteracting these effects.
Drug Interactions: Special caution should be observed when anileridine is used with other opioids, sedatives, some phenothiazines or anesthetics, since these agents may enhance respiratory and circulatory depression.
Adverse Reactions: Nausea and vomiting occur occasionally, and slight transient hypotension and bradycardia may be noted. Dizziness, perspiration, a feeling of warmth, dry mouth, visual difficulty, itching, euphoria, restlessness, nervousness and excitement have been reported.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: Primary attention should be given to the reestablishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation. Parenteral fluids and other supportive measures should be employed as indicated.
The opioid antagonist, naloxone HCl, is a specific antidote against respiratory depression.
An appropriate dose of naloxone HCl should be administered parenterally, preferably by the i.v. route and simultaneously with efforts at resuscitation. With anileridine overdosage the following treatment is recommended.
Naloxone HCl: Adults: 0.4 mg i.v., i.m. or s.c. If an immediate response is not observed the dose may be repeated at 2 to 3 minute intervals.
Children and Newborn: 0.01 mg/kg i.v., i.m. or s.c. may be repeated at 2 to 3 minute intervals.
Note: In a patient addicted to opioids, the use of an opioid antagonist may precipitate an acute withdrawal syndrome. The severity of this syndrome will depend on the amount of opioid which has been used and the amount of antagonist given.
Dosage And Administration: Oral: Adults: 25 to 50 mg, repeated every 6 hours if necessary. A dose of 50 mg, or more frequent repeat doses, may be desirable for extremely severe pain, but neither is advised for ambulatory patients outside of home or hospital.
Parenteral: S.C. and I.M.: Adults: 25 to 50 mg repeated every 4 to 6 hours. For more severe pain 75 to 100 mg may be given, and smaller, more frequent dosages may be necessary. The total 24 hour dosage of this drug should be no more than 200 mg.
When used preoperatively in adults, doses of 50 to 75 mg, especially when given with scopolamine, have made the patient drowsy and cooperative at induction of anesthesia.
I.V. use in support of anesthesia: Since the i.v. route is employed, anileridine should be used only in the hands of a competent anesthesiologist. During and directly following such use of the drug, provisions for oxygen administration and controlled respiration should be immediately available.
The drug frequently has been given i.v. without ill effect, but certain hazards nevertheless exist. The threshold of safety for a single i.v. dose of anileridine is relatively low and depends largely on the rate of administration. Severe respiratory depression has resulted from the i.v. injection of this analgesic during surgical anesthesia. As with similar agents, it may cause prolonged apnea when given rapidly i.v. in one dose. This effect is rare with a dose of 10 mg or less. Furthermore, it should be remembered that sedatives, other opioid analgesics, some phenothiazines and anesthetics may increase the likelihood of respiratory depression. If respiratory depression due to anileridine occurs, it may be reversed by naloxone.
Anileridine injection should be well diluted and introduced into the vein slowly. For adults, from 50 to 100 mg should be added to 500 mL of 5% dextrose solution, and 5 to 10 mg injected slowly followed by the amount desired at a relatively slow drip (approximately 0.6 mg/minute depending on individual need and response). The sudden injection of more than 10 mg may produce apnea, hypotension, and cardiac arrest. It has been reported that an adequate amount of drug, infused intermittently instead of continuously, has been effective for about 25 to 40 minutes.
Note: Direct i.v. injection of undiluted solution should not be employed except in grave emergency when time or facilities preclude dilution of the drug.
Parenteral Use in Obstetrics: For analgesia during labor, 50 mg of anileridine may be injected i.m. or s.c. If necessary this dose may be repeated, usually in 3 to 4 hours, for a total dosage of 100 to 200 mg. For rapid action 10 mg in dilution may be given i.v. slowly at the same time that 40 mg is injected i.m. or s.c.
Care should be taken at all times, and especially with i.v. use, to avoid opioid-induced respiratory depression of either the mother or the infant. Labor may be slowed in some instances and infant respiratory depression has been reported. Rarely is the depression marked. The closer to delivery the drug is given, the greater the likelihood of respiratory depression of the newborn.
Approximate Opioid Analgesic Equivalences: The potency of anileridine lies between that of meperidine and morphine, please refer to Table I for approximate analgesic equivalences of anileridine with respect to other opioid analgesics.
SuppliedSupplied: Tablets: Each white, biconvex-shaped, compressed tablet, 0.79 cm in diameter, with a special symbol on one side, contains: anileridine HCl equivalent to anileridine base 25 mg. Nonmedicinal ingredients: calcium phosphate dibasic, hydroxypropyl methylcellulose, magnesium stearate and sodium bisulfite. Gluten-, lactose- and tartrazine-free. Bottles of 100. Store at room temperature (15 to 30°C) and protect from light.
Injection: Each mL of clear, colorless liquid contains: anileridine phosphate 25 mg. Nonmedicinal ingredients: phosphoric acid, sodium bisulfite and water for injection. Ampuls of 1 mL, boxes of 25. Store at room temperature (15 to 30°C) and protect from excessive heat and light. (Shown in Product Recognition Section)
LERITINE® Injection LERITINE® Tablets Frosst Anileridine PhosphateAnileridine HCl Opioid Analgesic
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