CLI PHARMACY

CLINICAL PHARMACY

Topic: Drug Profile of Azithromycin

Submitted to: Sir Saleem

Submitted by: Anum Azam

Roll # 31

Semester 7th (M)

Department: Pharmacy

Govt. College University FSD

Name of the medicinal product:

 Azithromycin
Product Description
Sr. Dosage form Price Pack Size
Proprietary Manufacturer
NO. and strength
name
1 Aziromycin Nawan Cap 250mg 272 10's
Susp. 200mg/5ml 165 15ml
2 Azirol Harmann Tab. 250 mg 156 6's

3 Azure Fynk pharma Cap. 250 mg 250 10's

4 Caramycin Caraway Pharma Tab.250 mg 150 6's

5 Myzid cxarde Cap. 250mg 140 6's

Susp. 200mg/5ml 168 15ml
Cap. 250mg 398 12's
6 Azomax Novartis Pharma
Susp. 200mg/5ml 223.08 15ml
Tab.500mg 300 6's

Chemistry Of The Product

Chemical Class Structure Physical properties

Macrolide  White crystals

derivatives
 Melting point 114°C
 pH 0.2%
 Solution in a mixture
of methyl alcohol and
water(1:1) is between
9.0 and 11.0

Pharmacological properties
 Pharmacokinetics
Absorption:
Rapidly absorb.

Distribution:
Widely distributed in tissues then in plasma (up to 50 times max. observed conc. In
plasma) indicate highly tissue bound. Conc. In tissue like lungs, tonsils, prostate, exceed the MIC
90 for pathogens after a single dose of 500 mg.

Protein Placenta Secrete Volume of Therapeuti

Bioavailabilit Tmax BBB
bindin l barrier d in distributio c serum
y
g milk n level
Widely Poor 0.4-0.5mg/l
37% 7-5% Cross it Yes 2-3h.
distributed penetration of 500mg
in tissues dose.

Metabolism:

Site of metabolism Active Metabolites

Hepatic ----------------
Elimination:

Elimination half life Rout of excretion

2-4 days  Bile
 Feces
 urine

Pharmacodynamics

Therapeutic Class Pharmacodynamics Class Mechanism of action

Binds to 50s ribosomal subunit of

Antibiotic Protein synthesis inhibitor
susceptible bacteria and suppresses
(bacteriostatic)
protein synthesis

Preclinical Safety Data

In animal studies using exposures 40 times those achieved at the clinical therapeutic dosages,
Azithromycin was found to have caused reversible phospholipidosis, but as a rule there were no
associated toxicological consequences. The relevance of this finding to humans receiving
azithromycin in accordance with the recommendations is unknown.
Electrophysiological investigations have shown that azithromycin prolongs the QT interval.
Carcinogenic potential
Long-term studies in animals have not been performed to evaluate carcinogenic potential.
Mutagenic potential
There was no evidence of a potential for genetic and chromosome mutations in in vivo and in
vitro test models.
Reproductive toxicity
No teratogenic effects were observed in embryotoxicity studies in rats after oral administration
of azithromycin. In rats, azithromycin dosages of 100 and 200 mg/kg body weight/day led to
mild retardations in fetal ossification and in maternal weight gain. In peri- and postnatal studies
in rats, mild retardations following treatment with 50 mg/kg/day azithromycin and above were
observed.
Clinical Particulars

Indications Side effects

I nfection caused by susceptible organism
in lower respiratory tract infection including
bronchitis and pneumonia.
In upper respiratory tract infections
including otitis media, pharyngitis/tonsillitis
and sinusitis, skin and soft tissue infections
and acne, mild to moderate typhoid fever
caused by multidrug resistant strains.
In sexually transmitted diseases in men
and women.
Indicated in treatment of uncomplicated
genital infection due to chlamydia
trachomatis.
Is indicated as second line therapy for
typhoid fever caused by S.typhi, S. paratypi.
CVS: chest pain, palpitation, arrthymias.
CNS: dizziness, headache, vertigo, fever,
somnolence.
GIT: abdominal pain, nausea, vomiting,
cramping, diarrhoea.
Skin: photosensitivity, pruritus, rash,
urticaria, cutaneous vasculitis.
Hepatic: elevation in hepatic enzymes,
cholestatic jaundice.
Genitourinary: Monilia, vaginitis, nephritis.
Otic: ototoxicity, tinnitus.
Fatigue, allergic reaction rarely.
Sr. Duration of
Indication Recommended Dose in Adults
No therapy
.
1 Genital infection 1 g or 1000 mg given as a single dose
2 Pharyngitis and 500 mg given as single dose daily for 3 days. 3 days or 5
tonsillitis (Total dose 1.5 g). days
3 Skin infections 500 mg given as single dose daily for 3 days or 500 3 days or 5
mg given as single dose on 1st day of therapy days
followed by 250mg daily for 4 days.
(Total dose 1.5 g).
4 Pneumonia 500 mg given as single dose daily for 3 days or 500 3 days or 5
mg given as single dose on 1st day of therapy days
followed by 250mg daily for 4 days.
(Total dose 1.5 g).
5 Acute sinusitis 500 mg given as single dose daily for 3 days or 500 3 days or 5
mg given as single dose on 1st day of therapy days
followed by 250mg daily for 4 days.
(Total dose 1.5 g).
6 Typhoid fever Dose is 500 mg-1000 mg once daily 5-7 days

Dose in children
No data of dose on children under six month of age. The dose in children is 10 mg/kg as a single
dose for 3 days. For typhoid fever therapy should be given for 7 days.
Dose adjustment in renal impairment
No dose adjustment is needed in patients with mild renal impairment (Creatinine clearance
>40ml/min.). But there is no data regarding azithromycin usage in patients with more severe
renal impairment, thus caution should be taken in using azithromycin in these patients.
Dose adjustment in hepatic impairment
As liver is the principle route of excretion of azithromycin, it should not be used in patients with
hepatic disease.
Dose adjustment in pregnancy
Animal reproduction studies have demonstrated that azithromycin crosses placental barrier, but
no harm to the foetus. No data available for pregnant women and animal reproduction studies
Are not always predictive of human response, so it should be used during pregnancy if proper
alternative are not available.
Dose adjustment in lactation
No data on secretion of azithromycin in breast milk are available, so it should be in lactating
women where adequate alternative are not available.

Contraindications:
It is contraindicated in patients hypersensitive to azithromycin or any other compound of
formulation.

Precautions and warnings:

 Do not crush the capsules.
 Keep out of reach of children.
 If suspension shake well before use.
 It may cause superinfection so use it with caution.
 Use Azithromycin at least 1h. Before or 2h. After antacid.
 Serious allergic reactions including angioneurotic oedema and anaphylaxis are reported.

Drug-Drug Interaction

Sr. Interaction Outcomes Mechanism Recommendation

No

Penicillin Azithromycin may

1 Avoid concurrent use
inhibit antibacterial
activity of penicillin
Reduce peak serum Use at least 1h. Before or
2 Antacids
level 2h. after antacid

Cyclosporine Affected metabolism Avoid concurrent use, if

3
of Cyclosporine necessary monitor level
and adjust dose
Digoxin Elevated level Monitor
4

Ergot Toxicity of ergot

5 Avoid concurrent use
derivatives (ergotism)

Anticoagulant effect Metabolized via cyp Monitor

6 Warfarin may increase isoenzyme of warfarin

May increase toxic Monitor

7 Colchicine
effect of Colchicine
Increase Azithromycin
Neflinavir Monitor
8 serum level
 Drug- Food Interaction Drug-Lab interaction
Presence of food in GIT may affect the There are no lab test interactions reported.
extent of absorption of oral drug; however
the effect of food on absorption depends on
the dosage form administered.

Toxicology

Toxic dose Sign and Symptoms Management

If over dose is suspected,  Gastric lavage within
 Hearing lose
contact local poison control 1h.
canter or emergency room  Vomiting  Enhancement of
immediately.Maximum dose  Diarrhoea elimination: multiple
is 1500mg/d above it is dosing of charcoal.
considered as toxic.  Activated charcoal
may be effective

Effects on ability to drive & use machine

No studies on the effects on the ability to drive and use machines have been performed.
However, the possibility of undesirable effects like dizziness and convulsions should be taken
into account when performing these activities.

Direction for use

 Administer 1h before or 2h after meal.
 Tablets can be taken without regard of meal.
 Take medicine with 1 glass of water or noncitrus juice.
 Take dose at a proper time so therapeutic level can be achieved.
 Store reconstituted oral suspension at room temperature and use within 10 days. Discard
remaining after dosing is completed.
Preparation of suspension:
Shake the dry powder loose. Add the amount of water described below to the powder.
 For 15 ml (600 mg) bottle: add 7.5 ml water.
 For 20 ml (800 mg) bottle: add 10.0 ml water.
 For 22.5 ml (900 mg) bottle: add 11.0 ml water.
 For 30 ml (1200 mg) bottle: add 15.0 ml water.
 For 37.5 ml (1500 mg) bottle: add 18.5 ml water.
Shake well until a white to off white coloured, homogenous suspension is achieved. For
administration the syringe adapter should be placed in the neck of the bottle and the stopper
should be opened.
 Pharmaceutical particulars

Features Tablets Capsules Suspension

List of excipients Core Capsule contents Sucrose,
MCC, Pregelatinised maize Cellulose, MC, Xanthan gum,
starch, Sodium starch Sodium lauryl sulphate, Hydroxypropylcellulos,
Trisodium phosphate
glycolate, Colloidal anhydrous Magnesium stearate,
anhydrous, Silica, colloidal
silica, Sodium lauryl sulphate, Capsule Shell anhydrous,
Magnesium stearate. Gelatin, Aspartame,
Coating Titanium dioxide, Cream caramel, banana,
PVA, Titanium dioxide, Indigo carmine, cherry flavour,
Talc, Soya Lecithin, Sulphur dioxide. Titanium dioxide.
Xanthan Gum.
Incompatibilities Not applicable None known None known
Shelf life Close bottle with dry
3years 3 years
powder: 36 months.
Reconstituted suspension 5
days.
Storage Keep in tightly close container Do not store above Unopened bottle: Don’t
conditions store above 30 °C.
25°C.
Reconstituted suspension
Don’t store above 25 °C.
Instructions for No special requirements No special requirements Dose should be measured
storage and
with oral dosing syringe or
spoon. When dispensing
handling
22.5ml and 30ml packs,
advice correct usage of the
multi-dosing spoon.
Nature and PVC/PVDC/Alu. Blister pack PVC/PVDC/Alu. HDPE bottles with a PP/
contents of Pack sizes: Blister pack PE- childproof closure
container 500 mg: 2, 3, 6, 12, 24, 30, 50, Pack sizes: with retaining ring.
and 100 film-coated tablets 2, 4, 6 or 100 capsules. PE/PP-dosage syringe (10
Not all pack sizes may be Not all pack sizes may ml), graduated in 0.25 ml
marketed. be marketed. divisions.
Content of the bottle after
reconstitution: 15 ml (600
mg), 20 ml (800 mg), 22.5
ml (900 mg), 30 ml (1200
mg) or 37.5 ml (1500 mg).
REFERENCES
 http://www.doctorjeeves.com/product_artcle.php?id=116785.
 Pharmaguide, 20 Edition, Sep2009-2010.
 United State pharmacopeia (USP).
 British pharmacopeia (BP).
 British national formulary (BNF).