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Worksheets[PHARM] Endo 1 Prolactin drugs
Total questions: 21
Worksheet time: 11mins
A D2 receptor agonist and a semisynthetic ergot alkaloid which inhibits spontaneous and TRH-induced release of prolactin
Bromocriptine
Pergolide
Cabergoline
Quinagolide
• Half-life: 2-8 hours (short)
• Extensive first-pass hepatic metabolism
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Dosing
• Starting: 1.25 mg at bedtime with snacks
• After 1 week: morning dose of 1.25 mg may be added
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Indications
• For acromegaly at high doses
• For Parkinson’s disease at high doses
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Indications
First line of treatment for patients with prolactinomas who wish to become pregnant
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Indications
Decreases tumor size in >50% of patients
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Toxicity
• Nausea, vomiting
• Headache
• Postural hypotension
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Indications
• Less common: nasal congestion, psychosis, hallucinations, nightmare, insomnia
Bromocriptine
Pergolide
Cabergoline
Quinagolide
• Ergot derivative
• Least expensive
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Dosing
• Starting: 0.25 mg at bedtime
• Increased gradually to a max daily dose of 0.5 mg
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Indications
• Treatment of Parkinson’s disease
• Hyperprolactinemia (off-label)
Bromocriptine
Pergolide
Cabergoline
Quinagolide
• Longest duration of action
• Half-life: 65 hours
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Has higher affinity and 4x greater selectivity for the D2 receptor than Bromocriptine
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Dosing
• Initiated at 0.25 mg twice weekly or 0.5 mg once weekly orally or vaginally
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Indications
Treatment of hyperprolactinemia
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Toxicity
• Lower tendency to induce nausea, hypotension, and dizziness
• Safe in pregnant women with macroadenomas
Bromocriptine
Pergolide
Cabergoline
Quinagolide
• Newer non-ergot derivative with high D2 receptor affinity for hyperprolactinemia
• Half-life: 22 hours
Bromocriptine
Pergolide
Cabergoline
Quinagolide
Dosing
• Once daily dose of 0.1-0.5 mg/day
Bromocriptine
Pergolide
Cabergoline
Quinagolide
DOPAMINE AGONISTS
Bromocriptine
Cabergoline
Ergot derivatives
Non-ergot derivatives
DOPAMINE AGONISTS
Quinagolide
Pramipexole
Ropinirole
Ergot derivatives
Non-ergot derivatives
- Newer, non-ergot D2 agonist
- Used in Parkinson’s disease
- Reported to interfere with lactation, but are NOT approved for use in hyperprolactinemia
BROMOCRIPTINE and CABERGOLINE
QUINAGOLIDE
PRAMIPEXOLE and ROPINIROLE
