Drugs in our Pharmacy of Drugs in our Pharmacy of Natural Origin Natural Origin 1 1) Drugs Containing of Alkaloids ) Drugs Containing of Alkaloids
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 1/21
Drugs in our Pharmacy of Drugs in our Pharmacy of
Natural OriginNatural Origin
11) Drugs Containing of Alkaloids) Drugs Containing of Alkaloids
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 2/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 3/21
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 4/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 5/21
Chemical structureChemical structure
Ergotamine tartarate CaffeineErgotamine tartarate Caffeine
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 6/21
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).
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 7/21
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).).
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 8/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 9/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 10/21
Structure of Structure of ErgometrineErgometrine
NH
H
N
CH3
O
NH
OH
CH3
Ergometrine
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 11/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 12/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 13/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 14/21
Buscopan Dosage FormsBuscopan Dosage Forms
Typical dose is 10mg 3 times daily.for adults
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 15/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 16/21
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)
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 17/21
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.
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 18/21
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..
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 19/21
NH3
HO NH3
O
H CH2OH
O
(-)-Hyoscyami e
Atropi e
(-)-Hyosci e
Solanaceous Alkaloids
8/6/2019 Methyrgine Buscopan & Atropine (1)
http://slidepdf.com/reader/full/methyrgine-buscopan-atropine-1 20/21
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..