Cabaser
Cabaser - General Information
Cabaser, a lysergic acid amide derivative, is a potent dopamine receptor agonist on D2 receptors. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It is frequently used as a second-line agent in the management of prolactinomas when bromocriptine is ineffective. [Wikipedia]
Pharmacology of Cabaser
Cabaser is a dopamine receptor agonist and uncategorized drug which suppresses the production of prolactin in pituitary gland. It is an ergot-derivative. It has at times been used as an adjunct to SSRI antidepressants as there is some evidence that it counteracts certain side effects of those drugs such as reduced libido and anorgasmia. It also has been suggested online that it has a possible recreational use in reducing or eliminating the male refractory period.
Cabaser for patients
A patient should be instructed to notify her physician if she suspects she is pregnant, becomes pregnant, or intends to become pregnant during therapy. A pregnancy test should be done if there is any suspicion of pregnancy and continuation of treatment should be discussed with her physician.
Cabaser Interactions
DOSTINEX should not be administered concurrently with D2-antagonists, such as phenothiazines, butyrophenones, thioxanthines, or metoclopramide.
Cabaser Contraindications
DOSTINEX Tablets are contraindicated in patients with uncontrolled hypertension or known hypersensitivity to ergot derivatives.
Additional information about Cabaser
Cabaser Indication: For the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.
Mechanism Of Action: The secretion of prolactin by the anterior pituitary is mainly under hypothalmic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. Cabaser is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. Cabaser decreased serum prolactin levels in reserpinized rats. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1,- and α2- adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.
Drug Interactions: Erythromycin Erythromycin increases serum levels and toxicity of cabergoline
Food Interactions: Take with food to improve tolerance.
Absorption is not affected by food.
Generic Name: Cabergoline
Synonyms: Cabergolina [Spanish]; Cabergolinum [Latin]
Drug Category: Antineoplastic Agents; Antiparkinson Agents; Dopamine Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Cabergoline: Cabaser; Dostinex;
Absorption: First-pass effect is seen, however the absolute bioavailability is unknown.
Toxicity (Overdose): Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.
Protein Binding: Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner.
Biotransformation: Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal.
Half Life: The elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.
Dosage Forms of Cabaser: Tablet Oral
Chemical IUPAC Name: N-[3-(Dimethylamino)propyl]-N-[(ethylamino)carbonyl]- 6-(2-propenyl)-8g-ergoline-8-carboxamide
Chemical Formula: C26H37N5O2
Cabergoline on Wikipedia: https://en.wikipedia.org/wiki/Cabergoline
Organisms Affected: Humans and other mammals
