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Drug reference

lorcaserin

Selective serotonin 5-HT2C receptor agonist (anti-obesity; WITHDRAWN) · Weight management (historical use)

START
Use discouraged (withdrawn — cancer signal)
TYPICAL MAX
20 mg/day (historical ceiling)
STOP IF
Any signal of malignancy, serotonin syndrome, or depression
WATCH
Discontinue if <5% weight loss at 12 weeks; mood; not for use
CDSCO approvedATC A08AA11
Dose laddermg/d
10per dose20max/day
Renal dose adjustmenteGFR mL/min/1.73m²
CAUTIONUsual (no longer recommended in practice)30AVOIDNot recommended90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET1.8hPEAK11h12hDURATION
ONSET
1h · absorption
PEAK
1.8h · Tmax
11h ·
DURATION
12h · twice-daily
EXCRETION
Renal — mainly metabolites; ~3% unchanged
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Contraindicated.
FDA category + note
Top interactionssee all 12
  • AlfentanilSevereDatabaseDDInter
  • AlmotriptanSevereDatabaseDDInter
  • AmitriptylineSevereDatabaseDDInter
  • AmoxapineSevereDatabaseDDInter

Mechanism

Selective 5-HT2C receptor agonist on hypothalamic POMC neurons, reducing appetite and food intake; was used as adjunct to diet/exercise for weight loss until withdrawal.

Indications

Historical: chronic weight management (BMI ≥30, or ≥27 with comorbidity). WITHDRAWN from market (cancer signal in CAMELLIA-TIMI 61).

Dosing

Adult
Historical: 10 mg PO twice daily (or 20 mg ER once daily). Use discouraged/not available in most markets.
Pediatric
Not established.
Renal adjustment
Severe impairment: not recommended.
Hepatic adjustment
No specific adjustment for mild–moderate.
Geriatric
Limited data.
Max dose
20 mg/day (historical)

Pharmacokinetics

Onset
Appetite suppression within days
Peak effect
~1.5–2 h (Tmax)
Duration
~12 h (twice-daily)
Half-life
~11 h
Bioavailability
High
Protein binding
~70%
Metabolism
Hepatic (multiple pathways)
Excretion
Renal (mainly metabolites; ~3% unchanged)

Contraindications

  • Pregnancy
  • Hypersensitivity
  • Use generally not recommended (withdrawn)

Side effects

Common
HeadacheDizzinessNauseaDry mouthConstipationFatigue
Serious
  • Increased malignancy risk (cancer signal — withdrawal basis)
  • Serotonin syndrome (with serotonergic drugs)
  • Valvulopathy / pulmonary hypertension (theoretical, class)
  • Psychiatric (depression/suicidal ideation)
  • Hypoglycaemia (with diabetics)

Pregnancy & lactation

Pregnancy

Contraindicated.

Lactation

Avoid.

Drug interactions

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Almotriptan
Severe
Database

Clinical effect not specified

Source: DDInter

Amitriptyline
Severe
Database

Drug interaction classified as: synergy, metabolism

Source: DDInter

Amoxapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Benzphetamine
Severe
Database

Clinical effect not specified

Source: DDInter

Brexpiprazole
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Bromocriptine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Buspirone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cabergoline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Citalopram
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clomipramine
Severe
Database

Drug interaction classified as: synergy, metabolism

Source: DDInter

Desipramine
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

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Sources: Goodman & Gilman 14e·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20