Galantamine (Tablets, Capsules, Solution) Instructions for Use

Instructions
Dosage forms

ATC Code

N06DA04 (Galantamine)

Active Substance

Galantamine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Selective inhibitor of acetylcholinesterase in the brain. A drug for the treatment of Alzheimer’s disease

Pharmacotherapeutic Group

Dementia treatment agent

Pharmacological Action

Galantamine is a reversible cholinesterase inhibitor. It facilitates cholinergic transmission by enhancing and prolonging the action of endogenous acetylcholine.

It ensures neuromuscular transmission in skeletal muscles and exhibits antagonism towards non-depolarizing curare-like agents.

It increases the tone of smooth muscles of internal organs and enhances the secretion of exocrine glands.

It causes miosis, reduces intraocular pressure, and causes accommodation spasm.

It penetrates the blood-brain barrier well and enhances excitation processes in the cholinergic synapses of the central nervous system.

Pharmacokinetics

Galantamine is rapidly absorbed after subcutaneous administration. Therapeutic plasma concentration is achieved within 30 minutes.

The C_max in plasma after a single dose of 10 mg (oral and parenteral administration) is 1.2 mg/ml and is reached within 2 hours.

Galantamine is weakly bound to plasma proteins. It penetrates the blood-brain barrier well and is detected in brain tissues.

It is metabolized by demethylation (5-6%). Galantamine metabolites (epigalantamine and galantaminone) are detected in plasma and urine.

It is eliminated mainly by glomerular filtration. The elimination half-life is 5 hours. A small amount is excreted in bile (0.2±0.1%/24 h).

Galantamine unchanged and its metabolites (epigalantamine and galantaminone) are 89% excreted in the urine after subcutaneous administration. The renal clearance of galantamine is about 100 ml/min.

Indications

For oral administration: symptomatic treatment of mild to moderate dementia of the Alzheimer’s type.

For parenteral administration: poliomyelitis, neuritis, radiculitis, radiculoneuritis, polyneuritis, spastic paralysis, residual effects after cerebrovascular, toxic, and traumatic disorders (cerebral stroke, meningitis, meningoencephalitis, myelitis), myasthenia gravis, progressive muscular dystrophy, spinal and neural muscular atrophy; as an antagonist of non-depolarizing muscle relaxants.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
A80	Acute poliomyelitis
F00	Dementia in Alzheimer’s disease
G09	Sequelae of inflammatory diseases of the central nervous system
G12	Spinal muscular atrophy and related syndromes
G70.2	Congenital or acquired myasthenia
G71.0	Muscular dystrophy
G80.0	Spastic quadriplegic cerebral palsy
G81.1	Spastic hemiplegia
G82.1	Spastic paraplegia
G82.4	Spastic tetraplegia
I69	Sequelae of cerebrovascular diseases
M54.1	Radiculopathy
M79.2	Neuralgia and neuritis, unspecified
Y55.1	Muscle relaxants [skeletal muscle h-receptor blockers]

ICD-11 code	Indication
1C81	Acute poliomyelitis
1D0Z	Non-viral and unspecified infections of the central nervous system, unspecified
6D80.Z	Dementia due to Alzheimer’s disease, onset unknown or unspecified
6D8Z	Dementia, unknown or unspecified cause
8B25.Z	Sequelae of cerebrovascular disease, unspecified
8B61.Z	Spinal muscular atrophy, unspecified
8B93.Z	Radiculopathy, unspecified
8C61	Congenital myasthenic syndromes
8C70.Z	Muscular dystrophy, unspecified
8D20.10	Spastic tetraplegic cerebral palsy
8E4A.1	Paraneoplastic or autoimmune diseases of the peripheral or autonomic nervous system
FB56	Specified soft tissue diseases, not elsewhere classified
MB50.1	Spastic tetraplegia
MB53.2	Spastic hemiplegia
MB56	Paraplegia
PL00	Drugs, medicaments or biological substances causing injury or harm in therapeutic use

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Tablets, Capsules, Solution

For oral administration, the daily dose is 5-10 mg, frequency of administration is 3-4 times/day after meals, duration of treatment is 4-5 weeks. High doses are taken over a shorter period of time.

For subcutaneous administration, single doses for adults are 2.5-10 mg; for children aged 1-2 years – 0.25-0.5 mg, 3-5 years – 0.5-1 mg, 6-8 years – 0.75-2 mg, 9-11 years – 1.25-3 mg, 12-14 years – 1.75-5 mg, 15-16 years – 2-7 mg; if necessary, the dose can be increased, but strictly individually. For adults, the maximum single dose is 10 mg, the daily dose is 20 mg. Frequency of application is 1-2 times/day. Therapy is started with minimal doses, which are gradually increased; frequency of administration in high doses is 3 times/day. The course of treatment lasts up to 50 days; if necessary, 2-3 repeated courses can be conducted with an interval of 1-1.5 months.

For intravenous administration, single doses for adults are 10-25 mg; for children 1-2 years – 1-2 mg, 3-5 years – 1.5-3 mg, 6-8 years – 2-5 mg, 9-11 years – 3-8 mg, 12-15 years – 5-10 mg.

Adverse Reactions

From the digestive system: profuse salivation, nausea, vomiting.

Other: sweating, dizziness; rarely – bradycardia.

Contraindications

Bronchial asthma, bradycardia, angina pectoris, epilepsy, hyperkinesis, mechanical intestinal obstruction, mechanical impairment of urinary tract patency, severe hepatic impairment, severe renal impairment, children and adolescents under 18 years of age, hypersensitivity to galantamine.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

There are no clinical data on use during pregnancy. Experimental studies have revealed reproductive toxicity.

It is not known whether Galantamine is excreted in human breast milk.

Use in Hepatic Impairment

Contraindicated for use in severe hepatic impairment.

Use in Renal Impairment

Contraindicated for use in severe renal impairment.

Pediatric Use

Parenteral administration is possible according to the dosage regimen. Oral administration is contraindicated.

Geriatric Use

Use is possible according to the dosage regimen.

Special Precautions

In severe renal failure, the dose should be reduced. Treatment with galantamine should be carried out in combination with physiotherapeutic procedures, which should be started 1-2 hours after administration.

Drug Interactions

With simultaneous use with anticholinergic agents, antagonism towards the anticholinergic action is observed; with anticholinesterase agents and cholinomimetics – additive action.

With simultaneous use with inhibitors of CYP2D6, CYP3A4 isoenzymes, there is a possibility of increased side effects of galantamine.

With simultaneous use of ketoconazole, paroxetine, the bioavailability of galantamine increases.

With simultaneous use, there is a possibility of enhanced action of suxamethonium, due to the anticholinesterase effect of galantamine.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Galantamine [Atoll LLC (Russia)]
Film-coated tablets, 4 mg: from 10 to 500 pcs.
Film-coated tablets, 8 mg: from 10 to 500 pcs.
Film-coated tablets, 12 mg: from 10 to 500 pcs.

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Dosage Forms

	Galantamine	Film-coated tablets, 4 mg: from 10 to 500 pcs.
		Film-coated tablets, 8 mg: from 10 to 500 pcs.
		Film-coated tablets, 12 mg: from 10 to 500 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; the cross-section shows an almost white core and a film coating.

	1 tab.
Galantamine hydrobromide	5.126 mg
Equivalent to galantamine content	4 mg

Excipients: lactose monohydrate – 63.474 mg, microcrystalline cellulose (MCC-101) – 20 mg, croscarmellose sodium – 4 mg, povidone K25 – 3 mg, magnesium stearate – 0.9 mg, colloidal silicon dioxide – 0.5 mg.

Coating composition: hypromellose – 1.7 mg, titanium dioxide – 0.9 mg, macrogol-4000 – 0.4 mg.

From 10 to 50 pcs. – blister packs (from 1 to 10 pcs.) – cardboard packs.

Film-coated tablets white or almost white, round, biconvex, with a score; the cross-section shows an almost white core and a film coating.

	1 tab.
Galantamine hydrobromide	10.253 mg
Equivalent to galantamine content	8 mg

Excipients: lactose monohydrate – 126.947 mg, microcrystalline cellulose (MCC-101) – 40 mg, croscarmellose sodium – 8 mg, povidone K25 – 6 mg, magnesium stearate – 1.8 mg, colloidal silicon dioxide – 1 mg.

Coating composition: hypromellose – 3.4 mg, titanium dioxide – 1.8 mg, macrogol-4000 – 0.8 mg.

From 10 to 50 pcs. – blister packs (from 1 to 10 pcs.) – cardboard packs.

Film-coated tablets white or almost white, round, biconvex; the cross-section shows an almost white core and a film coating.

	1 tab.
Galantamine hydrobromide	15.38 mg
Equivalent to galantamine content	12 mg

Excipients: lactose monohydrate – 121.82 mg, microcrystalline cellulose (MCC-101) – 40 mg, croscarmellose sodium – 8 mg, povidone K25 – 6 mg, magnesium stearate – 1.8 mg, colloidal silicon dioxide – 1 mg.

Coating composition: hypromellose – 3.4 mg, titanium dioxide – 1.8 mg, macrogol-4000 – 0.8 mg.

From 10 to 50 pcs. – blister packs (from 1 to 10 pcs.) – cardboard packs.

Galantamine [Vifitech, CJSC (Russia)]
Solution for intravenous and subcutaneous administration 2.5 mg/ml: amp. 10 pcs.
Solution for intravenous and subcutaneous administration 10 mg/ml: amp. 10 pcs.

Marketing Authorization Holder

Vifitech, CJSC (Russia)

Dosage Forms

	Galantamine	Solution for intravenous and subcutaneous administration 2.5 mg/ml: amp. 10 pcs.
		Solution for intravenous and subcutaneous administration 10 mg/ml: amp. 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and subcutaneous administration transparent, colorless.

	1 amp.
Galantamine hydrobromide	2.5 g

Excipients: water for injections – up to 1000 ml.

1 ml – ampoules (5) – blister packs (2) – cardboard packs.
1 ml – ampoules (10) – cardboard packs.

Solution for intravenous and subcutaneous administration transparent, colorless.

	1 amp.
Galantamine hydrobromide	10 g

Excipients: water for injections – up to 1000 ml.

1 ml – ampoules (5) – blister packs (2) – cardboard packs.
1 ml – ampoules (10) – cardboard packs.

Galantamine [Vifitech, CJSC (Russia)]
Solution for intravenous and subcutaneous administration 5 mg/ml: 2 ml amp. 10 pcs.

Marketing Authorization Holder

Vifitech, CJSC (Russia)

Dosage Form

Galantamine

Solution for intravenous and subcutaneous administration 5 mg/ml: 2 ml amp. 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and subcutaneous administration	1 ml
Galantamine	5 mg

2 ml – ampoules (5) – blister packs (2) – cardboard packs.

Galantamine [Vifitech, CJSC (Russia)]
Solution for intravenous and subcutaneous administration 1 mg/ml: 10 ml amp. 10 pcs.

Marketing Authorization Holder

Vifitech, CJSC (Russia)

Dosage Form

Galantamine

Solution for intravenous and subcutaneous administration 1 mg/ml: 10 ml amp. 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and subcutaneous administration	1 ml
Galantamine	1 mg

10 ml – ampoules (5) – blister packs (2) – cardboard packs.

Galantamine Canon [Canonpharma Production, CJS (Russia)]
Extended-release capsules 8 mg: 7, 14, 28, 56, or 84 pcs.
Extended-release capsules 16 mg: 7, 14, 28, 56, or 84 pcs.
Extended-release capsules 24 mg: 7, 14, 28, 56, or 84 pcs.

Marketing Authorization Holder

Canonpharma Production, CJS (Russia)

Dosage Forms

	Galantamine Canon	Extended-release capsules 8 mg: 7, 14, 28, 56, or 84 pcs.
		Extended-release capsules 16 mg: 7, 14, 28, 56, or 84 pcs.
		Extended-release capsules 24 mg: 7, 14, 28, 56, or 84 pcs.

Dosage Form, Packaging, and Composition

Extended-release capsules hard gelatin No. 3, cap and body blue color; capsule contents – white or almost white spherical pellets.

	1 tab.
Galantamine hydrobromide	10.254 mg
Equivalent to galantamine content	8 mg

Excipients: hypromellose E5 – 2.46 mg, diethyl phthalate – 0.57 mg, microcrystalline cellulose – 84.43 mg, ethylcellulose – 2.29 mg, magnesium stearate – 0.5 mg, talc – 0.5 mg.

Hard gelatin capsule No.3:
Body – gelatin – 29.6341 mg, dye indigo carmine – 0.0207 mg, titanium dioxide – 0.6052 mg;
cap – gelatin – 17.3731 mg, dye indigo carmine – 0.0121 mg, titanium dioxide – 0.3548 mg.

7 pcs. – blister packs (1) – cardboard packs.
7 pcs. – blister packs (2) – cardboard packs.
7 pcs. – blister packs (4) – cardboard packs.
7 pcs. – blister packs (8) – cardboard packs.
7 pcs. – blister packs (12) – cardboard packs.

Extended-release capsules hard gelatin No. 3, cap and body blue color; capsule contents – white or almost white spherical pellets.

	1 tab.
Galantamine hydrobromide	20.508 mg
Equivalent to galantamine content	16 mg

Excipients: hypromellose E5 – 4.92 mg, diethyl phthalate – 1.14 mg, microcrystalline cellulose – 168.86 mg, ethylcellulose – 4.58 mg, magnesium stearate – 1 mg, talc – 1 mg.

Hard gelatin capsule No.2:
Body – gelatin – 37.2416 mg, dye indigo carmine – 0.1062 mg, dye patent blue V – 0.7622 mg;
cap – gelatin – 22.3684 mg, dye patent blue V – 0.0638 mg, titanium dioxide – 0.4578 mg.

Extended-release capsules hard gelatin No. 1, cap and body white color; capsule contents – white or almost white spherical pellets.

	1 tab.
Galantamine hydrobromide	30.761 mg
Equivalent to galantamine content	24 mg

Excipients: hypromellose E5 – 7.38 mg, diethyl phthalate – 1.71 mg, microcrystalline cellulose – 253.29 mg, ethylcellulose – 6.87 mg, magnesium stearate – 1.5 mg, talc – 1.5 mg.

Hard gelatin capsule size No.1:
Body – gelatin – 45.2956 mg, titanium dioxide – 0.9244 mg;
cap – gelatin – 29.1844 mg, titanium dioxide – 0.5956 mg.

7 pcs. – contour cell blisters (1) – carton packs.
7 pcs. – contour cell blisters (2) – carton packs.
7 pcs. – contour cell blisters (4) – carton packs.
7 pcs. – contour cell blisters (8) – carton packs.
7 pcs. – contour cell blisters (12) – carton packs.

Galantamine DS [Danson-BG (Bulgaria)]
Solution for injection 1 mg/ml: 1 ml amp. 5 or 10 pcs.
Solution for injection 5 mg/ml: 1 ml amp. 5 or 10 pcs.