apomorphine

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A poisonous white crystalline alkaloid, C₁₇H₁₇NO₂, derived from morphine and used medicinally to induce vomiting.

Brand names: Apokyn®Uprima™

Chemical formula:

Drug Forms:
• Apomorphine Hydrochloride Solution for injection (below)
• Apomorphine injection

Español:
• Clorhidrato de Apomorfina, Solución para inyección
• Inyección de apomorfina

Apomorphine Hydrochloride Solution for injection

What is this medicine?

APOMORPHINE (a poe MOR feen) is used to treat 'off' episodes in advanced Parkinson's disease. These episodes affect your ability to move or perform tasks.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•asthma or other breathing problems
•heart disease
•history of alcohol or drug abuse
•kidney or liver disease
•low blood pressure
•sleep disorder
•stroke
•an unusual or allergic reaction to apomorphine, sulfites, other medicines foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for injection under the skin. You will be taught how to prepare and give this medicine. You will also need to take a medicine to prevent nausea and vomiting for at least the first two months of therapy. Use exactly as directed. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.

It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•certain antibiotics like grepafloxacin and sparfloxacin
•cisapride
•medicines for irregular heart beat like amiodarone, disopyramide, dofetilide, flecainide, ibutilide, procainamide, quinidine, sotalol
•droperidol
•halofantrine
•levomethadyl
•pimozide
•some medicines for nausea like alosetron, dolasetron, dronabinol, droperidol, granisetron, ondansetron, palonosetron
•ziprasidone

This medicine may also interact with the following medications:
•alfuzosin
•certain antibiotics like clarithromycin, erythromycin, gatifloxacin, gemifloxacin, levofloxacin, moxifloxacin, troleandomycin
•medicines for high blood pressure or chest pain (angina)
•medicines to treat or prevent malaria like chloroquine or mefloquine
•metoclopramide
•phenothiazines like chlorpromazine, mesoridazine, prochlorperazine, thioridazine
•some medicines for depression like amitriptyline, amoxapine, maprotiline, mirtazapine, nefazodone, nortriptyline
•some medicines for mental disturbances like clozapine, haloperidol, molindone, olanzapine, pimozide, quetiapine, risperidone, ziprasidone

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress.
 
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. You may experience flushing, nausea, vomiting, pale skin, or sweating before dizziness or fainting occurs. Do not get up too quickly from a lying or sitting position. Report any dizziness or related symptoms to your health care provider as soon as possible. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks. Do not take any medications that cause drowsiness without first checking with your health care provider.
 
If you find that you have sudden feelings of wanting to sleep during normal activities, like cooking, watching television, or while driving or riding in a car, you should contact your health care professional.
 
This medicine may cause severe nausea and vomiting. Your doctor may prescribe a medication to prevent these symptoms. Do not treat yourself. Not all medicines for nausea and vomiting can be used with this medicine. Talk to your doctor about which one may be right for you.
 
There have been reports of increased sexual urges or other strong urges such as gambling while taking some medicines for Parkinson's disease. If you experience any of these urges while taking this medicine, you should report it to your health care provider as soon as possible.
 
You should check your skin often for changes to moles and new growths while taking this medicine. Call your doctor if you notice any of these changes.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•abnormal or unusual body movements
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•blood pressure changes
•confusion, hallucinations (seeing or hearing things that are not really there)
•depression or depressed mood
•difficulty breathing or swallowing
•dizziness or lightheadedness
•excess sweating
•fainting spells
•irregular or fast, pounding heartbeat, palpitations
•swelling in arms, hands, legs, or feet
•unusually weak or tired
•vomiting

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•drowsiness
•headache
•nausea
•yawning

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees). Throw away any unused medicine after the expiration date.

Last updated: 5/11/2004 11:36:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

An alkaloid from morphine. Used as the hydrochloride; administered parenterally it causes vomiting within 3 to 10 minutes but can also be administered orally. Stimulates receptors in the chemoreceptor trigger zone of the medulla oblongata.

Apomorphine
Systematic (IUPAC) name
(6aS)- 6-Methyl- 5,6,6a,7-tetrahydro- 4H-dibenzo [de,g] quinoline- 10,11-diol
Identifiers
CAS number	41372-20-7
ATC code	G04BE07 N04BC07
PubChem	6005
DrugBank	APRD00531
Chemical data
Formula	C17H17NO2
Mol. mass	267.322 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	100% following sc injection
Protein binding	~50%
Metabolism	hepatic
Half life	40 minutes (range 30-60 minutes)
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status	II (California), non-scheduled (Rest of USA)
Routes	sc

Apomorphine is a type of dopaminergic agonist (agonist of the D1 and D2 type dopamine receptors) ^[1], historically a morphine decomposition product by boiling with concentrated acid, hence the name. It does not actually contain morphine or its skeleton, or bind to opioid receptors. Apomorphine is a relatively non-selective dopamine receptor agonist, having possible slightly higher affinity for D₂-like dopamine receptors.

Historically, apomorphine has been tried for a variety of uses including psychiatric treatment of homosexuality in the early 20th century. Currently, apomorphine is used in the treatment of Parkinson's disease and (under the name Uprima) of erectile dysfunction. It was also successfully used in the treatment of heroin addiction, a purpose for which it was championed by the author William S. Burroughs. It is a potent emetic (i.e. it induces vomiting) and should not be administered without an antiemetic such as domperidone. The emetic properties of apomorphine are exploited in veterinary medicine to induce therapeutic emesis in canines that have recently ingested toxic or foreign substances.

For treatment of erectile dysfunction, it is believed that dopamine receptors in the hypothalamic region of the brain are the main target, as although dopamine receptors in the penis do facilitate erection, they do so far more weakly than those in the brain.^[2]

Apomorphine is colourless as a liquid but stains green. Therefore care must be taken to avoid splashes. Apormophine does not remain stable for more than 24 hours in a plastic container, so syringes are discarded if not used within 24 hours.

Contents 1 Use in Parkinson's disease 2 Erectile dysfunction 3 Alzheimer's disease 4 References 5 External links

Use in Parkinson's disease

First mooted as a treatment for Parkinson's disease as early as 1951,^[3] its clinical use was first reported in 1970 by Cotzias et al.,^[4] although its emetic properties and short half-life made oral use impractical. A later study found that combining the drug with the antiemetic domperidone improved results significantly.^[5]

Therapeutic use in Parkinson's disease is effective because of the drug's strong dopaminergic action, with a rapid effect (within 3–20 minutes of injection) but a brief duration.^[6] While apomorphine can be used in combination with l-dopa, the intention is usually to wean patients off of this, as by this stage they will probably be experiencing a great deal of dopa-induced dyskinesias and "off" periods.^[6] Following a successful apomorphine challenge, training of patient and caregiver, and careful dose titration, there is no reason why an apomorphine pump cannot be an effective monotherapy.^[6]

Erectile dysfunction

Apomorphine hydrochloride (trade name "Uprima") is used in the treatment of erectile dysfunction (male impotence). It is its mode of stimulating dopamine in the brain which is believed to enhance the sexual response. It was found to be of poor efficacy^[7] in a large-scale study by Researchers at the UK's Drug Safety Research Unit and University of Portsmouth and discontinued in the UK in January 2006.^[7] Around 65-70% of doctors felt it was ineffective, with 60% of over 11,000 patients (avg age 61) discontinuing in month 1 and a further 23% in month 2.^[7][8]

Alzheimer's disease

Apomorphine has been reported ^[9] to be an inhibitor of Beta amyloid fibril formation, and may thus have potential as a therapeutic for Alzheimer's disease

References

1. ^ Apomorphine-induced activation of dopamine receptors modulates FGF-2 expression in astrocytic cultures and promotes survival of dopaminergic neurons
2. ^ Matsumoto K, Yoshida M, Andersson K, Hedlund P (2005). "Effects in vitro and in vivo by apomorphine in the rat corpus cavernosum.". Br J Pharmacol 146 (2): 259–67. doi:10.1038/sj.bjp.0706317. PMID 16025145. 
3. ^ Schwab R, Amador L, Lettvin J. "Apomorphine in Parkinson's disease.". Trans Am Neurol Assoc 56: 251–3. PMID 14913646. 
4. ^ Cotzias G, Papavasiliou P, Fehling C, Kaufman B, Mena I (1970). "Similarities between neurologic effects of L-dopa and of apomorphine.". N Engl J Med 282 (1): 31–3. PMID 4901383. 
5. ^ Corsini G, Del Zompo M, Gessa G, Mangoni A (1979). "Therapeutic efficacy of apomorphine combined with an extracerebral inhibitor of dopamine receptors in Parkinson's disease.". Lancet 1 (8123): 954–6. doi:10.1016/S0140-6736(79)91725-2. PMID 87620. 
6. ^ ^{a b c} Chaudhuri K, Clough C (1998). "Subcutaneous apomorphine in Parkinson's disease.". BMJ 316 (7132): 641. PMID 9522772. http://bmj.bmjjournals.com/cgi/content/full/316/7132/641#B2. 
7. ^ ^{a b c} Pharmaceutical Business Review, "Study shows Abbott's Uprima ineffective for most UK patients"
8. ^ MedicineNet study review
9. ^ Lashuel HA, Hartley DM, Balakhaneh D, Aggarwal A, Teichberg S, Callaway DJE (2002). "New class of inhibitors of amyloid-beta fibril formation. Implications for the mechanism of pathogenesis in Alzheimer's disease". J Biol Chem 277 (45): 42881–42890. doi:10.1074/jbc.M206593200. PMID 12167652. http://www.jbc.org/cgi/content/abstract/277/45/42881. 

External links

• PDSP K_i database
• "Apomorphine - Frequently Asked Questions". Britannia Pharmaceuticals. http://www.apo-go.co.uk/faqs.shtm. 
• Andrew Lees and Kirsten Turner (2002). "Apomorphine for Parkinson’s Disease" (PDF). Practical Neurology 2: 280–287. doi:10.1046/j.1474-7766.2002.00086.x. http://pn.bmjjournals.com/cgi/reprint/2/5/280.pdf.  - Detailed usage guide for Apomorphine pumps for Parkinson's

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