Monograph
N04BC07 - Apomorphine |
Propably not porphyrinogenic |
PNP |
Rationale
Essentially non-Cyp metabolized morphine derivative very rapidly cleared (< 1 h) from the circulation. Pharmacokinetic Cyp-dependent drug interactions with apomorphine as perpetrator are unlikely.
Potentially porphyrogenic nausea and vomiting may prevented by careful antiemetic premedication by domperidone. Dopamine-antagonistic phenothiazine antiemetics or metoclopramide are not to be used.
Chemical description
Dibenzokinoline morphine derivative with structural similarities to dopamine. Administered as the hydrochloride.
Therapeutic characteristics
Apomorphine is used in the acute treatment of motoric off-periods in MbParkinson. Administered after thorough antiemetic premedication. Administered acutely during hypokinetic (motoric off)-period of Mb parkinson. Administered subcutaneously due to poor oral bioavailability as it undergoes extensive first pass metabolism. Only to be used in in-hospital care in the hands of specialists. Apomorphine stimulates dopaminergic postsynaptic receptor sites by way of dopamine receptor D1 and D2 agonism.
Physiological effects of possible relevance to acute porphyria: results from in vitro tests suggests that apomorphine may influence the secretion of pituitary hormones which may in turn have an effect on the regulation of CYP enzymes, but the clinical relevance is uncertain.
Metabolism and pharmacokinetics
Well absorbed after s.c. injection, with rapid (4-12 min) onset of action, and short (1 h) duration of effect. The only recognized clearance pathway is renal excretion after glucuronidation and sulphonation. In vitro studies have shown inhibition of CYP1A2, 2D6 and 3A4, but only for concentrations well above clinical relevance.
References
# | Citation details | PMID |
---|---|---|
* | Scientific articles | |
1. | 2001 Oct;88 Suppl 3:18-21.
Argiolas A, Hedlund H, et al. The pharmacology and clinical pharmacokinetics of apomorphine SL. BJU Int. |
|
2. | The role of the nervous system in the regulation of liver cytochrome p450.
Wójcikowski J, Daniel WA, et al. Curr Drug Metab. 2011 Feb;12(2):124-38. |
|
* | Drug reference publications | |
3. | Sweetman SC, editor. Martindale: The complete drug reference. Apomorphine (19.06.2012).
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|
* | Summary of Product Characteristics | |
4. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Apomorphine.
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Similar drugs
Tradenames and packages
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Netherlands
APO-go · APO-go 5 mg/ml, oplossing voor infusie in een voorgevulde spuit · APO-go Ampullen 10 mg/ml oplossing voor injectie of infusie · APO-go Pod 5 mg/ml oplossing voor infusie in een patroon · APO-go PEN · APO-go PEN 10 mg/ml oplossing voor injectie · Apomorfine · Apomorfine hydrochloride PharmSwed 5 mg/ml, oplossing voor infusie · Dacepton · Dacepton 10 mg/ml oplossing voor injectie / infusie · Dacepton 10 mg/ml oplossing voor injectie in een patroon · Dacepton 5 mg/ml oplossing voor infusieBelgium
APO-GO-PEN · APO-GO-PEN 10 mg/ml sol. inj. s.c. cart. · Apomorphine · Apomorphine HCl Sterop 5 mg/ml sol. inj./perf. s.c. amp. · Dacepton · Dacepton 10 mg/ml sol. inj. s.c. cart. · Dacepton 5 mg/ml sol. perf. s.c. flac.United Kingdom
APO-go · APO-go 20mg/2ml solution for injection ampoules · APO-go 50mg/5ml solution for injection ampoules · APO-go PEN · APO-go PEN 30mg/3ml solution for injection · APO-go PFS · APO-go PFS 50mg/10ml solution for infusion pre-filled syringes · APO-go POD · APO-go POD 100mg/20ml solution for infusion cartridges · Apomorphine · Apomorphine 100mg/20ml solution for infusion pre-filled syringes · Apomorphine 20mg/2ml solution for injection ampoules · Apomorphine 2mg/2ml solution for injection ampoules · Apomorphine 50mg/5ml solution for injection ampoules · Dacepton · Dacepton 100mg/20ml solution for infusion vials · Dacepton 30mg/3ml solution for injection cartridgesDenmark
APO-go · APO-go POD · APO-go Pumpfill · APO-go Pen · Apomorfin · Apomorfin "PharmSwed" · DaceptonNorway
Apomorfin PharmSwed · Britaject · DaceptonPoland
DaceptonLuxembourg
APO-GO-AMP · APO-GO-PEN · DaceptonFinland
Apogo Pen · Apomorphine Stada · DaceptonLatvia
APO-go PEN · Apomorphine · Apomorphine Kalceks · Dacepton
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