Names and pronunciation
(roh-pin′ih-role) Requip, Requip XL
PDF page 1180
Loading InternPractice…
Drug reference
(roh-pin′ih-role) Requip, Requip XL
PDF page 1180
Func. class.: Antiparkinson agent
PDF page 1180
Chem. class.: DOPamine-receptor agonist, nonergot
PDF page 1180
Do not confuse: rOPINIRole/risperiDONE
PDF page 1180
ACTION: Selective agonist for D2 re- ceptors (presynaptic/postsynaptic sites); binding at D3 receptor contributes to antiparkinson effects
PDF page 1180
USES: Parkinson’s disease, restless legs syndrome (RLS)
PDF page 1180
CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, dysrhythmias, affective disorder, psychosis, cardiac/ renal/hepatic disease
PDF pages 1180, 1181
SIDE EFFECTS CNS: Agitation, insomnia, psychosis, hallucination, dystonia, depression, diz- ziness, somnolence, sleep attacks, impulse control disorders CV: Orthostatic hypotension, tachycardia, hypo/hypertension, syncope, palpitations EENT: Blurred vision GI: Nausea, vomiting, anorexia, dry mouth, constipation, dyspepsia, flatulence GU: Impotence, urinary frequency HEMA: Hemolytic anemia, leukopenia, agranulocytosis INTEG: Rash, sweating RESP: Pharyngitis, rhinitis, sinusitis, bronchitis, dyspnea
PDF page 1181
INTERACTIONS Increase: rOPINIRole effect—cimeti- dine, ciprofloxacin, diltiaZEM, enoxacin, erythromycin, fluvoxaMINE, mexiletine, norfloxacin, tacrine, digoxin, theophyl- line, l-dopa Decrease: rOPINIRole effects—butyro- phenones, metoclopramide, phenothi- azines, thioxanthenes
PDF page 1181
DOSAGE AND ROUTES Parkinson’s disease • Adult: PO (regular release) 0.25 mg tid × 1 wk; gradually titrate at weekly intervals: Week 2, 0.5 mg tid; Week 3, 0.75 mg tid; Week 4, 1 mg tid; After week 4, may increase by 1.5 mg/day each week, max 9 mg/day total dosage, and then by 3 mg/day each week, max 24 mg/day • PO (ext rel) 2 mg/day × 1-2 wk, may increase by mg/day at intervals ≥1 wk based upon response; max 24 mg/day; if significant interruption of therapy oc- curs, retitration may be necessary Restless legs syndrome • Adult: PO (reg rel) 0.25 mg daily 1-3 hr before bedtime; days 3-7, may increase to 0.5 mg daily; at the beginning of week 2 (day 8), the dosage may be increased to 1 mg daily × 1 wk; weeks 3-6, dosage may be titrated up by 0.5 mg each week (from 1.5-3 mg over the 5-wk period) as needed to achieve desired effect
PDF page 1181
Available forms: Tabs 0.25, 0.5, 1, 2, 3, 4, 5 mg; ext rel tab 2, 4, 6, 8, 12 mg
PDF page 1181
Administer: • Product until NPO before surgery • Adjust dosage to patient response; ta- per when discontinuing • With meals to reduce nausea • Extended release: do not chew, crush, or divide • Testing for diabetes mellitus, acro- megaly if patient receiving long-term therapy
PDF page 1181
Assess: • Parkinsonism: akinesia, tremors, stag- gering gait, muscle rigidity, drooling • B/P, respirations during initial treatment; hypo/hypertension should be reported • Sleep attacks: drowsiness, falling asleep without warning even during haz- ardous activities • Mental status: affect, mood, behavioral R changes, depression; complete suicide assessment; worsening of symptoms in restless legs syndrome • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; avoid breast- feeding, excretion unknown
PDF page 1181
Evaluate: • Therapeutic response: improvement in movement disorder
PDF page 1181
CLINICAL CONSIDERATIONS
PDF page 1181
Patient and caregiver information: • To notify prescriber if pregnancy is planned or suspected, or if breast feeding • To take with food to prevent nausea • To report hallucinations, confusion (usually in geriatric patients) • That therapeutic effects may take sev- eral weeks to a few months • To change positions slowly to prevent orthostatic hypotension • To report any suspicious skin le- sions; that dermatologic or skin exami- nations should be performed regularly due to risk of melanoma in Parkinson’s patients • To use product exactly as prescribed; that if product is discontinued abruptly, parkinsonian crisis may occur; that prod- uct will be titrated weekly • That drowsiness, sleep attacks may occur; to avoid driving, other hazardous activities until response known • To avoid alcohol, CNS depressants, cough and cold products • To notify prescriber if unusual urges occur HIGH ALERT
PDF pages 1181, 1182
PHARMACOKINETICS Peak 1-2 hr, half-life 6 hr, extensively metabolized by liver by P450 CYP1A2 enzyme system, protein binding 40%
PDF page 1181
• Adult: PO (regular release) 0.25 mg tid × 1 wk; gradually titrate at weekly intervals: Week 2, 0.5 mg tid; Week 3, 0.75 mg tid; Week 4, 1 mg tid; After week 4, may increase by 1.5 mg/day each week, max 9 mg/day total dosage, and then by 3 mg/day each week, max 24 mg/day
PDF page 1181
• PO (ext rel) 2 mg/day × 1-2 wk, may increase by mg/day at intervals ≥1 wk based upon response; max 24 mg/day; if significant interruption of therapy oc- curs, retitration may be necessary Restless legs syndrome
PDF page 1181
• Adult: PO (reg rel) 0.25 mg daily 1-3 hr before bedtime; days 3-7, may increase to 0.5 mg daily; at the beginning of week 2 (day 8), the dosage may be increased to 1 mg daily × 1 wk; weeks 3-6, dosage may be titrated up by 0.5 mg each week (from 1.5-3 mg over the 5-wk period) as needed to achieve desired effect
PDF page 1181