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Galantamine

 
Drug Info: Galantamine
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Brand names: Razadyne™Razadyne™ERReminyl™ ERReminyl®

Chemical formula:



Galantamine extended-release caspules

What are galantamine extended-release caspules?

GALANTAMINE (Razadyne® ER) helps treat the symptoms associated with Alzheimer's disease. It is not a cure for Alzheimer's disease but offers improvement in memory, attention, reason, language, and the ability to perform tasks. Benefits are greater in the early stages of the disease. Generic galantamine extended-release capsules are not yet available.

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 lung disease
• difficulty passing urine
• head injury
• heart disease, or irregular or slow heartbeat
• kidney disease
• liver disease
• low blood pressure
• Parkinson's disease
• seizures (convulsions)
• stomach or intestinal disease, ulcers, or stomach bleeding
• an unusual or allergic reaction to galantamine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take galantamine extended-release capsules by mouth. Follow the directions on the prescription label. Swallow with a drink of water. Take just once daily, preferably in the morning. Taking the medication with food and plenty of liquid may help lessen side effects such as upset stomach. Do not chew, crush or cut the capsules. Take your doses at regular intervals. Do not take your medicine more often than directed. Continue to take your medicine even if you feel better. Do not stop taking except on your prescriber's advice. Dose increases should not occur more often than every 4 weeks; follow your prescriber's dose recommendations.

If therapy has been stopped for several days or more, your prescriber will restart your therapy at a lower dose.

Following your prescriber's dosing and administration directions may help avoid the most common adverse effects.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, take it as soon as you can. Only take this medicine once per day. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What drug(s) may interact with galantamine?

• amantadine
• atropine
• benztropine
• bosentan
• carbamazepine
• clarithromycin
• cimetidine
• dicyclomine
• digoxin
• donepezil
• erythromycin
• glycopyrrolate
• hyoscyamine
• medications for fungal infections (fluconazole, itraconazole, ketoconazole, terbinafine)
• medications for motion sickness (examples: dimenhydrinate, meclizine, scopolamine)
• medications for Parkinson's disease
• medicines that relax your muscles for surgery
• non-steroidal anti-inflammatory drugs (examples: ibuprofen, naproxen)
• oxybutynin
• phenobarbital
• phenytoin
• propantheline
• rifampin, rifabutin, or rifapentine
• rivastigmine
• some medications for depression, anxiety or mood disorders
• some medications for heart disease or high blood pressure
• some medications for HIV infection
• St. John's wort
• tacrine
• tolterodine
• troglitazone

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking galantamine?

Visit your prescriber or health care professional for regular checks on your progress. Check with your prescriber or health care professional if there is no improvement in your symptoms or if they get worse.

You may get dizzy or feel faint. Do not drive, use machinery, or do anything that needs mental alertness until you know how galantamine affects you.

If you are going to have surgery tell your prescriber or health care professional that you are taking galantamine.

What side effects may I notice from taking galantamine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• changes in vision or balance
• diarrhea, if it is severe or does not stop
• difficulty breathing
• difficulty or pain when urinating
• dizziness, fainting spells, or falls
• nervousness, agitation, or increased confusion
• skin rash or hives
• slow heartbeat, or palpitations
• stomach pain
• uncontrollable movements
• vomiting
• weight loss

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• mild diarrhea, especially when starting treatment
• drowsiness
• headache
• indigestion or heartburn
• loss of appetite
• nausea
• tiredness
• trembling
• trouble sleeping

Where can I keep my medicine?

Keep out of reach of children in a container that small children cannot open.

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

Last updated: 5/2/2005 10:08:00 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.

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Wikipedia: Galantamine
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Home > Library > Miscellaneous > Wikipedia
Galantamine
Systematic (IUPAC) name
(4aS,6R,8aS)- 5,6,9,10,11,12- hexahydro- 3-methoxy- 11-methyl- 4aH- [1]benzofuro[3a,3,2-ef] [2] benzazepin- 6-ol
Identifiers
CAS number 357-70-0
ATC code N06DA04
PubChem 9651
DrugBank APRD00206
ChemSpider 3331
Chemical data
Formula C17H21NO3 
Mol. mass 287.354 g/mol
Pharmacokinetic data
Bioavailability 80 to 100%
Protein binding 18%
Metabolism Hepatic partially CYP450:CYP2D6/3A4 substrate
Half life 7 hours
Excretion Renal (95%, of which 32% unchanged), fecal (5%)
Therapeutic considerations
Pregnancy cat.

B
Legal status

Rx and OTC
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Galantamine (Nivalin, Razadyne, Razadyne ER, Reminyl) is a chemical used for the treatment of mild to moderate Alzheimer’s disease and various memory impairments. It is an alkaloid that is obtained synthetically or from the bulbs and flowers of the Caucasian snowdrop (Voronov’s snowdrop), Galanthus woronowii (Amaryllidaceae) and related genera like Narcissus (daffodil), Leucojum (snowflake) and Lycoris including Lycoris radiata (Red Spider Lily). The active ingredient was isolated by prof. Paskov 1959 (Sopharma, Bulgaria) from a species tradionally used as a popular medicine in Eastern Europe and thus the idea for developing a medicine from these species seems to be based on the local use (ie, an ethnobotany-driven drug discovery).[1][2] It has been used for decades in Eastern Europe esp. in the symptomatic treatment of polio (poliomyelitis) and was later developed by Janssen Pharmaceutica into an Alzheimer medication. In the US it has been sold as a dietary supplement for memory and dream support prior to being approved as a drug by the FDA.

Contents

Pharmacology

Galantamine in its pure form is a white powder. Galantamine is a competitive and reversible cholinesterase inhibitor. It is believed it works by enhancing cholinergic function by increasing the concentration of acetylcholine in the brain. The atomic resolution 3D structure of the complex of galantamine and its target, acetylcholinesterase, was determined by X-ray crystallography in 1999 (PDB code: 1DX6; see complex).[3] There is no evidence that galantamine alters the course of the underlying dementing process.[4] Galantamine has also shown activity in modulating the nicotinic cholinergic receptors to increase acetylcholine release.[5]

Pharmacokinetics

Absorption of galantamine is rapid and complete and shows linear pharmacokinetics. It is well absorbed with absolute oral bioavailability between 80 and 100%. It has a half-life of seven hours. Peak effect of inhibiting acetylcholinesterase was achieved about one hour after a single oral dose of 8 mg in some healthy volunteers.

Plasma protein binding of galantamine is about 18%, which is relatively low.

Metabolism

The major route of metabolism for galantamine is through the liver, this accounts for approximately 75% of the total metabolism of galantamine. Hepatic cytochrome P450 (CYP) isoenzymes are the active enzymes for this metabolic route. In vitro studies have shown that CYP2D6 and CYP3A4 are involved in galantamine metabolism.

For Razadyne ER (the once-a-day formulation), CYP2D6 poor metabolizers had drug exposures that were approximately 50% higher than for extensive metabolizers. About 7% of the population has this genetic mutation, however because the drug is individually titrated to tolerability, no specific dosage adjustment is necessary for this population.

Clinical use

Indications

Galantamine is indicated for mild to moderate Vascular Dementia and Alzheimer's.[6][7]

Available forms

The product is supplied in twice-a-day tablets, once-a-day extended release capsules, and in oral solution. The tablets come in 4 mg, 8 mg, and 12 mg forms. The capsules come in 8 mg, 16 mg, and 24 mg forms.

Adverse events

In clinical trials, galantamine's side effect profile was very similar to that of other cholinesterase inhibitors, with gastrointestinal symptoms being the most notable and most commonly observed. In practice, some other cholinesterase inhibitors might be better tolerated; however, a careful and gradual titration over more than three months may lead to equivalent long-term tolerability.[8]

Other use

Supplement for lucid dream and out-of-body experience

Some people who practice lucid dream (LD) or out-of-body experience (OBE) use galantamine to increase their odds to achieve LD or OBE.[9][10][11] By taking small amount of galantamine (around 4 to 8 mg) after five to six hours of deep sleep and practice an induction technique such as meditation, MILD or WILD [2] many people report more success with galantamine.[12]

There are also reports that taking galantamine without proper induction technique will not lead to LD or OBE but will result in only a vivid dream instead. It should also be noted that due to a long half life Galantamine will stay in the body for a period of up to and over 48 hours, as such it is advisable to space out the use of Galantamine over a period of three days so that the body does not build a resistance to the drug ruining its effectiveness.[9]

Galantamine used with choline bitartrate or Alpha-GPC can dramatically increase one's odds of becoming lucid and increase memory consolidation during dreaming.[citation needed] Some people report mixing galantamine with other nootropic can enhance the degree of lucidity, but this is still controversial since some mixtures may work for some people, but lead to failure for others.

Nootropic

Along with other cholinergics or acetylcholinesterase inhibitors such as Huperzine A, galantamine also has been used as nootropic or "brain enhancer" to enhance memory in brain-damaged adults.[13]

Caution

The U.S. Food and Drug Administration (FDA) and international health authorities have published an alert based on data from two studies during the treatment by galantamine of mild cognitive impairment; higher mortality rates were seen in drug-treated patients.[14] On April 27, 2006, FDA approved labeling changes concerning all form of galantamine preparations (liquid, regular tablets,and extended release tablets) warning of the risk of bradycardia (and sometimes atrioventricular block,especially in predisposed persons). At the same time, the risk of syncope seems to be increased relative to placebo.[15] These side effects have not been reported in any other studies except in mild cognitive impairment.

Total synthesis

Main article: Galanthamine total synthesis

Galantamine is produced from natural resources and a patented total synthesis process. Many other synthetic methods exist but have not been implemented on an industrial scale.

References

  1. ^ Heinrich, M. and H.L. Teoh (2004) Galanthamine from snowdrop – the development of a modern drug against Alzheimer's disease from local Caucasian knowledge. Journal of Ethnopharmacology 92: 147 – 162. (doi:10.1016/j.jep.2004.02.012)
  2. ^ Scott LJ, Goa KL. Adis Review: Galantamine: a review of its use in Alzheimer's disease. Drugs 2000;60(5):1095-122 PMID 11129124
  3. ^ Greenblatt, HM, Kryger, G, Lewis, T, Silman, I, Sussman, JL "Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3Å resolution" FEBS Lett 1999; 463, 321-26. PMID 10606746
  4. ^ Ortho-McNeil Neurologics, "Razadyne ER US Product Insert", May 2006. [1]
  5. ^ Woodruff-Pak DS, Vogel RW 3rd, Wenk GL, "Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning" Proc Natl Acad Sci U S A. 2001 Feb 13;98(4):2089-94. PMID 11172080
  6. ^ Galantamine Benefits Both Alzheimer’s Disease and Vascular Dementia
  7. ^ Galantamine Improves Attention in Alzheimer's
  8. ^ Birks J. "Cholinesterase inhibitors for Alzheimer's disease." Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005593. PMID 16437532
  9. ^ a b Thomas Yuschak (2006). Advanced Lucid Dreaming (1st ed.). Lulu Enterprises. ISBN 978-1-4303-0542-2. 
  10. ^ Thomas Yuschak (2007). Pharmacological Induction of Lucid dreams. http://www.advancedld.com/f/Pharmacological_Induction_of_Lucid_Dreams.pdf. 
  11. ^ "Substances that enhance recall and lucidity during dreaming". Stephen LaBerge - US Patent. http://www.freepatentsonline.com/20040266659.html. Retrieved 2007-10-29. 
  12. ^ "Galantamine LDS Profile". Yuschak LDS Profiles. http://www.advancedld.com/galantamine.html. Retrieved 2007-10-29. 
  13. ^ Galantamine Protects Neurons and Memory Following Brain Injury
  14. ^ "FDA ALERT: Galantamine hydrobromide (marketed as Razadyne, formerly Reminyl) - Healthcare Professional Sheet". Postmarket Drug Safety Information for Patients and Providers. Food and Drug Administration. March 2005. http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm126140.htm. Retrieved 2009-07-30. 
  15. ^ "Safety Labeling Changes Approved By FDA Center for Drug Evaluation and Research (CDER)". MedWatch, The FDA Safety Information and Adverse Event Reporting Program. Food and Drug Administration. April 2006. Archived from the original on 2007-10-09. http://web.archive.org/web/20071009145003/http://www.fda.gov/medwatch/safety/2006/apr06.htm. Retrieved 2009-07-30. 

External links

v • d • e
Parasympathomimetics / cholinergic agonists / acetylcholinesterase inhibitors (N06DA, N07AA)
Direct
(at receptor)
Indirect/AIs
(in synapse)

very short acting: Edrophonium

carbamates/stigmine: Ambenonium · Rivastigmine · Distigmine · tertiary/CNS (Physostigmine) · quaternary/peripheral (Neostigmine, Pyridostigmine)

anti-dementia (Galantamine, Donepezil, Tacrine)
v • d • e
Psychoanaleptics: anti-dementia drugs (N06D)
Anticholinesterases

Tacrine · Donepezil · Rivastigmine · Galantamine
Other

This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 
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