Drugs in our Pharmacy of Natural Origin 1) Drugs Containing of Alkaloids.

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Drugs in our Drugs in our Pharmacy of Natural Pharmacy of Natural Origin Origin 1) Drugs Containing of 1) Drugs Containing of Alkaloids Alkaloids

Transcript of Drugs in our Pharmacy of Natural Origin 1) Drugs Containing of Alkaloids.

Page 1: Drugs in our Pharmacy of Natural Origin 1) Drugs Containing of Alkaloids.

Drugs in our Pharmacy of Drugs in our Pharmacy of Natural OriginNatural Origin

1) Drugs Containing of Alkaloids1) Drugs Containing of Alkaloids

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1) Cafergot1) Cafergot

Generic Name: caffeine and ergotamine Generic Name: caffeine and ergotamine Brand Names: Brand Names: Cafatine, Cafergot, Cafetrate, Cafatine, Cafergot, Cafetrate, Ercaf, Migergot, WigraineErcaf, Migergot, Wigraine

Caffeine and ergotamine both cause Caffeine and ergotamine both cause vasoconstriction (narrowing) of arteries and vasoconstriction (narrowing) of arteries and veins that supply blood to the head.veins that supply blood to the head.

Caffeine and ergotamine are used to prevent Caffeine and ergotamine are used to prevent and to treat vascular headaches such as and to treat vascular headaches such as migraine and migraine-like headaches.migraine and migraine-like headaches.

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CAFERGOTCAFERGOT

Each tablet for oral administration contains Each tablet for oral administration contains 1 mg ergotamine tartrate, USP, and 100 mg 1 mg ergotamine tartrate, USP, and 100 mg

caffeine, USP.caffeine, USP. Inactive ingredients include acacia, calcium Inactive ingredients include acacia, calcium

carbonate, compressible sugar, carbonate, compressible sugar, confectioner's sugar (sucrose and corn confectioner's sugar (sucrose and corn starch), magnesium stearate, methylparaben, starch), magnesium stearate, methylparaben, microcrystalline cellulose, povidone, microcrystalline cellulose, povidone, propylparaben, sodium benzoate, sodium propylparaben, sodium benzoate, sodium starch glycolate, starch (potato), sucrose, starch glycolate, starch (potato), sucrose, synthetic iron oxide, titanium dioxide and synthetic iron oxide, titanium dioxide and other ingredients.other ingredients.

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Chemical structureChemical structure

Ergotamine tartarate CaffeineErgotamine tartarate Caffeine

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Natural source of Caffeine:* Coffee consists of the dried ripe seed of Coffea arabica or other

Coffea species (Rubiaceae).

* Tea is the prepared leaves and leaf buds of Camellia sinensis

(Thea sinensis) (Theaceae).

* Cola, or kola, is the dried cotyledon from seeds of various

species of Cola e.g. C. nitida and C. acuminata (Sterculiaceae).

* Cocoa (or cacao) is derived from the roasted seeds of

Theobroma cacao (Sterculiaceae).

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Natural Source of ErgotamineNatural Source of Ergotamine

Ergotamine is an alkaloid isolated from Ergotamine is an alkaloid isolated from ergot. Ergot is the dried sclerotium of ergot. Ergot is the dried sclerotium of the fungus the fungus Claviceps purpurea Claviceps purpurea (Clavicipitaceae) developed on the (Clavicipitaceae) developed on the ovary of rye, ovary of rye, Secale cereale Secale cereale (Graminae). (Graminae).

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Uses of ErgotamineUses of Ergotamine

ErgotamineErgotamine is used in the treatment of is used in the treatment of acute attacks of acute attacks of migrainemigraine, Ergotamine , Ergotamine is effective orally, or by inhalation in is effective orally, or by inhalation in aerosol form, and may be combined aerosol form, and may be combined with caffeine. with caffeine.

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2) Methergine2) Methergine

Ergometrine is used as an Oxytocic , and is injected Ergometrine is used as an Oxytocic , and is injected

during the final stages of labour and immediately during the final stages of labour and immediately

following childbirth, especially if haemorrhage following childbirth, especially if haemorrhage

occurs.occurs.

Bleeding is reduced because of its vasoconstrictor Bleeding is reduced because of its vasoconstrictor

effects, and it is valuable after Caesarian operations. effects, and it is valuable after Caesarian operations.

* Ergometrine is also orally active. It produces * Ergometrine is also orally active. It produces

stimulation of uterine muscles.stimulation of uterine muscles.

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Structure of ErgometrineStructure of Ergometrine

NH

HN

CH3O

NHOH

CH3

Ergometrine

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LSDLSD

Lysergic acid diethyl amide is a semi-Lysergic acid diethyl amide is a semi-synthetic Compound prepared from synthetic Compound prepared from lysergic acid.lysergic acid.

It is a powerful hallucinogen.It is a powerful hallucinogen.

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ErgotismErgotism

It is a poisonous case resulting from It is a poisonous case resulting from the chronic consumption of rye or the chronic consumption of rye or wheat flour contaminated with ergot. wheat flour contaminated with ergot. Alkaloids of ergot cause Alkaloids of ergot cause vasoconstriction especially in the vasoconstriction especially in the limbs, that may results by time in limbs, that may results by time in gangrene of one or more limbs.gangrene of one or more limbs.

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3) Buscopan3) Buscopan Buscopan tablets contain the active ingredient hyoscine-Buscopan tablets contain the active ingredient hyoscine-

N-butylbromide, which is an antispasmodic alkaloid. It is N-butylbromide, which is an antispasmodic alkaloid. It is used to relieve abdominal pain that is caused by painful used to relieve abdominal pain that is caused by painful spasms in the muscles of the gastrointestinal (GI) or spasms in the muscles of the gastrointestinal (GI) or genitourinary (GU) tract.genitourinary (GU) tract.

Hyoscine stops the spasms in the smooth muscle by Hyoscine stops the spasms in the smooth muscle by preventing acetylcholine from acting on the muscle. It preventing acetylcholine from acting on the muscle. It does this by blocking the receptors on the muscle cells does this by blocking the receptors on the muscle cells that the acetylcholine would normally act on. that the acetylcholine would normally act on.

By preventing acetylcholine from acting on the muscle in By preventing acetylcholine from acting on the muscle in the GI and GU tracts, hyoscine reduces the muscle the GI and GU tracts, hyoscine reduces the muscle contractions. This allows the muscle to relax and contractions. This allows the muscle to relax and reduces the painful spasms and cramps.reduces the painful spasms and cramps.

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Buscopan Dosage FormsBuscopan Dosage Forms

Typical dose is 10mg 3 times daily.for adults

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Side effectsSide effects

Dry mouth. Dry mouth. Blurred vision. Blurred vision. Reduced ability to sweat. Reduced ability to sweat. Increase in heart rate (tachycardia). Increase in heart rate (tachycardia). Constipation. Constipation. Allergic skin reactions.Allergic skin reactions.

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4) Atropine4) Atropine

Atropine is a Atropine is a corecore medicine in the medicine in the World Health Organization's "'s "Essential Drugs List", which is a list of minimum ", which is a list of minimum medical needs for a basic health care system.medical needs for a basic health care system.

Atropine is a Atropine is a racemic mixture of D- mixture of D-hyoscyamine and L-hyoscyamine.and L-hyoscyamine.

The most common atropine compound used in The most common atropine compound used in medicine is atropine medicine is atropine sulfate . .

Atropine sulfate Injection, USP Atropine sulfate Injection, USP 0.1 mg/mI (Adult) 0.1 mg/mI (Adult) 0.05 mg/mL (Pediatric) 0.05 mg/mL (Pediatric)

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Pharmacological Action of AtropinePharmacological Action of Atropine

A mydriatic (causes dilatation of the eye pupil).

An antispasmodic (relaxes the intestinal and bronchial smooth muscles).

A preanesthetic medication to stop body

secretions. A CNS stimulant. An antidote to organophosphorus

insecticides.

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Side Effects of AtropineSide Effects of Atropine

Adverse reactions to atropine include: Adverse reactions to atropine include: ventricular ventricular fibrillation. . tachycardia.. dizziness. . nnausea. . blurred vision & dilated pupilsblurred vision & dilated pupils loss of balance, & loss of balance, & confusion..

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NH3C

O

O

HO NH3C

O

H CH2OH

O

(-)-Hyoscyamine

Atropine

(-)-Hyoscine

Solanaceous Alkaloids

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Natural Source of Atropine & Natural Source of Atropine & HyoscineHyoscine

AtropineAtropine & Hyoscine are & Hyoscine are tropane alkaloids extracted from s extracted from deadly nightshade ((Atropa belladonnaAtropa belladonna), ), jimsonweed ( (Datura Datura stramoniumstramonium), Duboisia(), Duboisia(Duboisia Duboisia myobroides)myobroides), henbane (, henbane (hyoscyamus niger hyoscyamus niger & hyoscyamus muticus& hyoscyamus muticus) and other plants ) and other plants of the family of the family Solanaceae..

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Natural Sources of Atropine & Natural Sources of Atropine & Hyoscine Hyoscine

Atropa belladonna( Solanaceae)

Hyoscyamus niger( Solanaceae)

Datura stramonium