Sansert

SANSERT- methysergide maleate tablet, coated
Novartis Pharmaceuticals Corporation

T2000-69

89011201

Information for the physician

Sansert ®

(methysergide maleate) tablets, USP

Rx only

Prescribing Information

WARNING

Retroperitoneal Fibrosis, Pleuropulmonary Fibrosis and Fibrotic Thickening of Cardiac Valves May Occur in Patients Receiving Long-term Methysergide Maleate Therapy. Therefore, This Preparation Must Be Reserved for Prophylaxis in Patients Whose Vascular Headaches Are Frequent and/or Severe and Uncontrollable and Who Are Under Close Medical Supervision.
(See also WARNINGS section)

DESCRIPTION

Sansert® (methysergide maleate) is a partially synthetic compound structurally related to lysergic acid butanolamide, well-known as methylergonovine in obstetrical practice as an oxytocic agent.

Chemically, methysergide maleate is designated as ergoline-8-carboxamide, 9,10-didehydro-N -[1-(hydroxymethyl)propyl]-1,6-dimethyl-, (8ß)-, (Z)-2-butenedioate (1:1) (salt).

Its structural formula is:

Image from Drug Label Content

Methylation in the number 1 position of the ring structure enormously enhances the antagonism to serotonin which is present to a much lesser degree in the partially methylated compound (methylergonovine maleate) as well as profoundly altering other pharmacologic properties.

Active Ingredient: methysergide maleate, USP.

Inactive Ingredients: acacia, carnauba wax, colloidal silicon dioxide, FD&C Blue #1, FD&C Yellow #5, gelatin, lactose, malic acid, povidone, sodium benzoate, starch (corn), stearic acid, sucrose, synthetic black iron oxide, talc, and titanium dioxide.

ACTIONS

Sansert® (methysergide maleate) has been shown, in vitro and in vivo , to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a “headache substance” acting directly or indirectly to lower pain threshold (others in this category include tyramine; polypeptides, such as bradykinin; histamine; and acetylcholine), as an intrinsic “motor hormone” of the gastrointestinal tract, and as a “hormone” involved in connective tissue reparative processes. Suggestions have been made by investigators as to the mechanism whereby methysergide produces its clinical effects, but this has not been finally established.

INDICATIONS

For the prevention or reduction of intensity and frequency of vascular headaches in the following kinds of patients:

  1. Patients suffering from one or more severe vascular headaches per week.
  2. Patients suffering from vascular headaches that are uncontrollable or so severe that preventive therapy is indicated regardless of the frequency of the attack.

CONTRAINDICATIONS

Hypersensitivity to the drug or to tartrazine (FD&C Yellow #5) or any other components of the formulation, pregnancy, lactation, peripheral vascular disease, severe arteriosclerosis, severe hypertension, coronary artery disease, phlebitis or cellulitis of the lower limbs, pulmonary disease, collagen diseases or fibrotic processes, impaired liver or renal function, valvular heart disease, debilitated states and serious infections.

WARNINGS

With long-term, uninterrupted administration, retroperitoneal fibrosis or related conditions — pleuropulmonary fibrosis and cardiovascular disorders with murmurs or vascular bruits have been reported. Patients must be warned to report immediately the following symptoms and to discontinue the drug: cold, numb, and painful hands and feet; leg cramps on walking; any type of girdle, flank, or chest pain, shortness of breath, or any associated symptomatology. Should any of these symptoms develop, methysergide should be discontinued. Continuous administration should not exceed 6 months. There must be a drug-free interval of 3-4 weeks after each 6-month course of treatment. The dosage should be reduced gradually during the last 2-3 weeks of each treatment course to avoid “headache rebound.”

The drug is not recommended for use in children.

PRECAUTIONS

General

All patients receiving Sansert® (methysergide maleate) should remain under constant supervision of the physician and be examined regularly for the development of fibrotic or vascular complications. (See ADVERSE REACTIONS)

The manifestations of retroperitoneal fibrosis, pleuropulmonary fibrosis, and vascular shutdown have shown a high incidence of regression once Sansert® (methysergide maleate) is withdrawn. These facts should be borne in mind to avoid unnecessary surgical intervention. Cardiac murmurs, which may indicate endocardial fibrosis, have shown varying degrees of regression, with complete disappearance in some and persistence in others.

Sansert® (methysergide maleate) has been specifically designed for the prophylaxis of vascular headache and has no place in the management of the acute attack.

Sansert® (methysergide maleate) tablets contain FD&C Yellow No. 5 (tartrazine) which may cause allergic-type reactions (including bronchial asthma) in certain susceptible individuals. Although the overall incidence of FD&C Yellow No. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity.

Information for Patients

Sansert® (methysergide maleate) is intended for use as a preventive agent in the treatment of vascular headaches. It should not be used for acute migraine attacks. If, after a 3-week trial period, Sansert® (methysergide maleate) has not been effective in decreasing the frequency or intensity of headaches, it is unlikely that longer administration of Sansert® (methysergide maleate) will be beneficial.

Patients should be advised to report the following symptoms immediately and to discontinue the drug: cold, numb, and painful hands and feet; leg cramps on walking; any type of girdle, flank, or chest pain; shortness of breath; or any associated symptomatology. There must be a drug-free interval of 3-4 weeks after each 6-month course of treatment.

Sansert® (methysergide maleate) should be taken with meals. Weight gain may necessitate modification of diet.

Drug Interactions

Methysergide may reverse the analgesic activity of narcotic analgesics. Concurrent use with vasoconstrictor agents including ergot alkaloids, sumatriptan, and nicotine (e.g. smoking) may result in enhanced vasoconstriction.

Pregnancy Category X

Sansert® (methysergide maleate) is contraindicated in pregnancy due to its oxytocic actions.

Nursing Mothers

There are no specific studies on the use of Sansert® (methysergide maleate) in nursing mothers. Ergot alkaloids, in general, appear in mothers’ milk.

Sansert® (methysergide maleate) is a semi-synthetic compound structurally related to ergotamine, and thus it may appear in breast milk. Ergot alkaloids have been reported to cause nausea, vomiting, diarrhea and weakness in the nursing infant and suppression of prolactin secretion and lactation in the mother.

Because of the potential for serious adverse reactions in nursing infants from Sansert® (methysergide maleate), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

ADVERSE REACTIONS

Within the recommended dose levels, the following side effects have been reported:

1) Fibrotic Complications

Fibrotic changes have been observed in the retroperitoneal, pleuropulmonary, cardiac, and other tissues, either singly or, very rarely, in combination.

Retroperitoneal Fibrosis

This nonspecific fibrotic process is usually confined to the retroperitoneal connective tissue above the pelvic brim and may present clinically with one or more symptoms such as general malaise, fatigue, weight loss, backache, low grade fever (elevated sedimentation rate), urinary obstruction (girdle or flank pain, dysuria, polyuria, oliguria, elevated BUN), vascular insufficiency of the lower limbs (leg pain, Leriche syndrome, edema of legs, thrombophlebitis). The single most useful diagnostic procedure in suspected cases of retroperitoneal fibrosis is intravenous pyelography. Typical deviation and obstruction of one or both ureters may be observed.

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