Methyrgine Buscopan & Atropine (1)

8/6/2019 Methyrgine Buscopan & Atropine (1)

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Drugs in our Pharmacy of Drugs in our Pharmacy of

Natural OriginNatural Origin

11) Drugs Containing of Alkaloids) Drugs Containing of Alkaloids



1) Cafergot1) Cafergot

Generic Name: caffeine and ergotamineGeneric Name: caffeine and ergotamine

Brand Names:Brand Names: CafatineCafatine,, Cafergot Cafergot,, CafetrateCafetrate,,

Ercaf Ercaf,, Migergot Migergot,, WigraineWigraine

Caffeine and ergotamine both causeCaffeine 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 asand to treat vascular headaches such as

migraine and migrainemigraine and migraine- -like headaches.like headaches.



CAFERGOTCAFERGOT

Each tablet for oral administration containsEach tablet for oral administration contains

1 mg ergotamine tartrate, USP, and 100 mg1 mg ergotamine tartrate, USP, and 100 mgcaffeine, USP.caffeine, USP.

Inactive ingredients include acacia, calciumInactive ingredients include acacia, calciumcarbonate, compressible sugar,carbonate, compressible sugar,confectioner's sugar (sucrose and cornconfectioner's sugar (sucrose and cornstarch), magnesium stearate, methylparaben,starch), magnesium stearate, methylparaben,microcrystalline cellulose, povidone,microcrystalline cellulose, povidone,

propylparaben, sodium benzoate, sodiumpropylparaben, sodium benzoate, sodiumstarch glycolate, starch (potato), sucrose,starch glycolate, starch (potato), sucrose,synthetic iron oxide, titanium dioxide andsynthetic iron oxide, titanium dioxide andother ingredients.other ingredients.



Chemical structureChemical structure

Ergotamine tartarate CaffeineErgotamine tartarate Caffeine



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).



Natural Source of ErgotamineNatural Source of Ergotamine

Ergotamine is an alkaloid isolated fromErgotamine is an alkaloid isolated from

ergot. Ergot is the driedergot. Ergot is the dried sclerotiumsclerotium of of

the fungusthe fungus ClavicepsClaviceps purpurea purpurea((ClavicipitaceaeClavicipitaceae) developed on the) developed on the

ovary of rye,ovary of rye, SecaleSecale cerealecereale ((GraminaeGraminae).).



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,, ErgotamineErgotamine

is effective orally, or by inhalation inis effective orally, or by inhalation inaerosol form, and may be combinedaerosol form, and may be combined

with caffeine.with caffeine.



2) Methergine2) Methergine

ErgometrineErgometrine is used as anis used as an OxytocicOxytocic , and is injected, and is injected

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

following childbirth, especially if following childbirth, especially if haemorrhagehaemorrhageoccurs.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.

** ErgometrineErgometrine is also orally active. It producesis also orally active. It produces

stimulation of uterine muscles.stimulation of uterine muscles.



Structure of Structure of ErgometrineErgometrine

NH

H

N

CH3

O

NH

OH

CH3

Ergometrine



LSDLSD

Lysergic acid diethyl amide is a semiLysergic acid diethyl amide is a semi--

synthetic Compound prepared fromsynthetic Compound prepared from

lysergic acid.lysergic acid.

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



ErgotismErgotism

It is a poisonous case resulting fromIt 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 causeAlkaloids of ergot cause

vasoconstriction especially in thevasoconstriction especially in the

limbs, that may results by time inlimbs, that may results by time in

gangrene of one or more limbs.gangrene of one or more limbs.



33) Buscopan) Buscopan

Buscopan tablets contain the active ingredient hyoscineBuscopan tablets contain the active ingredient hyoscine--NN--butylbromide, which is an antispasmodic alkaloid. It isbutylbromide, which is an antispasmodic alkaloid. It isused to relieve abdominal pain that is caused by painfulused to relieve abdominal pain that is caused by painfulspasms 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 byHyoscine stops the spasms in the smooth muscle by

preventing acetylcholine from acting on the muscle. Itpreventing acetylcholine from acting on the muscle. Itdoes this by blocking the receptors on the muscle cellsdoes this by blocking the receptors on the muscle cellsthat the acetylcholine would normally act on.that the acetylcholine would normally act on.

By preventing acetylcholine from acting on the muscle inBy preventing acetylcholine from acting on the muscle inthe GI and GU tracts, hyoscine reduces the musclethe GI and GU tracts, hyoscine reduces the musclecontractions. This allows the muscle to relax andcontractions. This allows the muscle to relax andreduces the painful spasms and cramps.reduces the painful spasms and cramps.



Buscopan Dosage FormsBuscopan Dosage Forms

Typical dose is 10mg 3 times daily.for adults



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.



44) Atropine) Atropine

Atropine is a Atropine is a corecore medicine in themedicine in the World HealthWorld HealthOrganizationOrganization's "'s "Essential Drugs ListEssential Drugs List", which is a", which is alist of minimum medical needs for a basic healthlist of minimum medical needs for a basic healthcare system.care system.

Atropine is a Atropine is a racemicracemic mixture of Dmixture of D--hyoscyaminehyoscyamineand Land L--hyoscyamine.hyoscyamine.

The most common atropine compound used inThe most common atropine compound used in

medicine is atropinemedicine is atropine sulfatesulfate .. Atropine sulfate Injection, USPAtropine sulfate Injection, USP

0.1 mg/mI (Adult)0.1 mg/mI (Adult)0.05 mg/mL (Pediatric)0.05 mg/mL (Pediatric)



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.



Side Effects of AtropineSide Effects of Atropine

Adverse reactions to atropine include: Adverse reactions to atropine include:

ventricular ventricular fibrillationfibrillation..

tachycardiatachycardia.. dizzinessdizziness..

nnauseaausea..

blurred vision & dilated pupilsblurred vision & dilated pupils loss of balance, &loss of balance, & confusionconfusion..



NH3

HO NH3

O

H CH2OH

O

(-)-Hyoscyami e

Atropi e

(-)-Hyosci e

Solanaceous Alkaloids



Natural Source of Atropine &Natural Source of Atropine &

HyoscineHyoscineAtropineAtropine & Hyoscine are& Hyoscine are tropanetropane

alkaloidalkaloids extracted froms extracted from deadly nightshadedeadly nightshade

(( At ropa belladonna At ropa belladonna),), jimsonweed jimsonweed ((DaturaDatura

st ramoni umst ramoni um), Duboisia(), Duboisia(DuboisiaDuboisia

myobroides)myobroides), henbane (, henbane (hyoscyamus niger hyoscyamus niger

& hyoscyamus mut ic us& hyoscyamus mut ic us) and other plants) and other plants

of the familyof the family SolanaceaeSolanaceae..



Natural Sources of Atropine &Natural Sources of Atropine &

HyoscineHyoscine

At ropa belladonna

( Solanaceae)

Hyoscyamus niger ( Solanaceae)

Datura stramonium

Methyrgine Buscopan & Atropine (1)

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