Bismillah-Hir-Rahmanir Rahim

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Welcome to Virtual
Presentation
of

Antiamoebic drug:
Metronidazole

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Presented by:
Group A
Presenter:
Simom Hasan BPH040100028
Members:
Md. Kamaruzzaman
BPH040100013
Tanvir Ahamed BPH040100021
Md. Moniruzzaman
BPH040100024
Md. Jahid Masud BPH040100027
Department of Pharmacy
Northern University Bangladesh.
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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Antiamoebic drug:

The drugs which act against amoeba or other

protozoa.

Examples:
Metronidazole
Diloxanide

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Metronidazole
Physical Info:
Appearance : White or yellowish, crystalline,
powder.

Solubility : Slightly soluble in water,

acetone, alcohol
and methylene chloride.

Dilution : Dissolve 1.0 g in 1M HCl &

dilute in 20 ml

Melting point : 158°C to 160°C.

Partition Coefficient: -0.02 at 25°C

(octanol/water).

Loss on drying maximum 0.5 per cent

Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
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 Metronidazole
Chemical Info:

IUPAC name : 2-(2-methyl-5-nitro-1H-imidazol-

1-yl)ethanol.
Chemical Formula : C6H9N3O3
Molecular Weight : 171.15 g/mol
Biological Half-life : 6 to 12 hours.
Chemical Half-life : 4 to 16 hours.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
Chemical Structure:

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
3D Chemical Structure:

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
Structural Similarity

Metronidazole Tinidazole

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Mechanism of
Action:
• Metronidazole enters
an aerobic bacterium

• Ferrodoxin is reduced
by electron transport.

• The drug then binds

to DNA, and DNA
breakage occurs.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Contraindicatio
ns:
• Hypersensitivity to Metronidazole or
other nitroimidazole derivatives.
• Patients with active neurological
disorders or a history of blood
dyscrasia.
• Trichomoniasis infections in the first
trimester of pregnancy and it crosses the
placental barrier.
• Metronidazole is distributed into milk.
Breast-feeding can be resumed 24 to 48
hours after treatment.
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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Risk Groups at a
glance:

Pregnant women Children Nursing mothers

Elderly people Renal failure Liver insufficiency

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Metronidazole
Precautions:

In the treatment of trichomoniasis:

To minimize the risk of re infection and

transmission:
- abstain from intercourse.
Or - to use a condom during intercourse
for the duration of treatment.

- If one is contaminated, treatment

will apply to both.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Precautions
:

Transient eosinophilia and leukopenia have

been observed during treatment with
metronidazole.

Treatment with metronidazole should be

discontinued if ataxia or any other symptom of
CNS involvement occurs.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
Drug interactions:

Alcohol : Warned consuming alcohol (during therapy and

for 24 hours post-treatment) because of a possible
disulfiram-like reaction.

Anticoagulants: Potentiate anticoagulant effect of

warfarin resulting in a prolongation of prothrombin
time.

Barbiturates: Metabolism may be enhanced, causing

reduced serum concentrations.
Disulfiram : Administering together may result in
confusion and psychotic reactions because of
combined toxicity.
Lithium: Initiation therapy has been associated with
increased serum lithium levels and, in a few cases,
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Groupsigns of lithiumBPH040100021,
A: BPH040100013, toxicity.BPH040100024, BPH040100027,
 Metronidazole
Adverse
Effects:
Cardiovascular: Palpitation and Chest Pain.

CNS: Peripheral Neuropathy, Convulsive Seizures,

Transient Ataxia, Dizziness, Drowsiness,
Confusion, Insomnia and Headache.

Dermatologic: Rash and Pruritus. With topical use:

Dry kin, Skin Irritation, Stinging or Burning of the
skin.

Metabolic: Gynecomastia has been reported rarely.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
Adverse Effects:

Gastrointestinal: Diarrhea, Nausea, Vomiting,

Unpleasant Metallic Taste, Anorexia,
Epigastric Distress, Dyspepsia, Constipation,
Dry Mouth, Glossitis, Stomatitis, Candidiasis
(oral).

Hematologic: Transient Eosinophilia or

Leukopenia.

Hypersensitivity: Erythematous Rash, Urticaria,

Serum Sickness-like reactions have been
reported rarely.

Local Reactions: Thrombophlebitis has occurred

with i.v. administration. 17
Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Metronidazole
Overdose:

Symptoms:
- Severe toxicity following overdosage with
metronidazole is uncommon.
- Massive ingestion may cause vomiting,
nausea, anorexia and headache.
- Insomnia, drowsiness, depression and
darkening of urine may also occur.

Treatment: There is no specific antidote.

Symptomatic and supportive therapy is
usually sufficient.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
Dosage forms:

Metronidazole is available as:

- Injection
- Oral Capsules and Tablets
- Vaginal gel and Inserts
- Cream or Gel.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Doses:
Adults:
Oral: 500 mg every 8 hrs,
(7.5 mg/kg every 6 to 8 hrs),
maximum: 4 g/24 hrs.
I.V.: 500 mg by i.v. infusion every 8 hrs,
(7.5 mg/kg every 6 to 8 hrs)
maximum: 4 g/24 hrs.

Children: 30 mg/kg/day i.v. in 3 divided doses or

15 to 30 mg/kg/day orally in 3 to 4 divided doses.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Treatments:

Amebiasis:
Adults:
Acute intestinal amebiasis or amebic hepatic
abscess: 750 mg 3 times daily for 10 days.
Treatment should be followed with a course of
a luminal amebicide

Children:
35 to 50 mg/kg/day in 3 divided doses for 10
days.
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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
enetration of the blood-brain barrier by metronidazol

In human volunteers, 90 min after oral metronidazole

(2.4 g), the average CSF/serum ratio of biologically
active metronidazole was 0.43. The lowest CSF
concentrations were several fold higher than those
needed to inhibit Bacteroides fragilis in vitro. These
results encourage clinical trials of metronidazole in the
treatment of central nervous system infections
caused by anaerobic bacteria or amoebae.

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Metronidazole

Some other information about Metronidazole:

Spectrum of activity:
- Anaerobic gram-negative bacilli
- Fusobacterium and Veillonella
- anaerobic gram-positive Cocci
- Eubacterium, Peptococcus and
- Peptostreptococcus
- H. pylori, G. vaginalis, E. histolytica,
- T. vaginalis, G. lamblia.

Metronidazole is not active against fungi,

viruses.
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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Metronidazole
Pharmacokinetics:
In Oral Administration:
- well absorbed from the gastrointestinal tract
- Peak serum levels in 1 to 2 hours.
In Topical Administration:
- serum levels 0.75% gel to the skin.

less than 20% of metronidazole bound to

serum proteins and is widely distributed in
the body.
Excreted primarily in the urine as metabolites
with 20% of a dose excreted as unchanged drug.
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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
References:
Internet Searching:
www.wikipedia.com
www.rxmed.com
www.rxlist.com
www.3dchem.com
Online Drug Bank

(http://redpoll.pharmacy.ualberta.ca/drugbank/)

British Pharmacopoeia 2002 (CD version)

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,
 Thanks for being with us

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Group A: BPH040100013, BPH040100021, BPH040100024, BPH040100027,