COMPOSITION
Each capsule contains:
Doxycycline hydrochloride equivalent to Doxycycline 100 mg.
PHARMACOLOGICAL CLASSIFICATION
Broad- and medium-spectrum antibiotic.
PHARMACOLOGICAL ACTION
Doxycycline is a bacteriostatic antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, resulting in the inhibition of protein synthesis.
It is bacteriostatic against a wide range of Gram-positive and Gram-negative organisms.
Doxycycline has demonstrated in vitro activity against the following organisms (although in vitro activity does not necessarily imply clinical efficacy):
Vibrio cholerae
Ureaplasma urealyticum
Mycoplasma pneumoniae
Chlamydia trachomatis
Chlamydia psittaci
Borrelia recurrentis
Calymmatobacterium granulomatis
Borrelia burgdorferi
Penicillin-sensitive Neisseria gonorrhoeae
Rickettsiae
PHARMACOKINETICS
Doxycycline is readily and almost completely absorbed from the gastrointestinal tract. Absorption is not significantly affected by food or milk.
Following a single oral dose of 200 mg, peak plasma concentrations of approximately 2.6 micrograms/mL are achieved within about 2 hours, decreasing to approximately 1.45 micrograms/mL after 24 hours.
Following intravenous administration of the same dose, peak plasma concentrations are initially higher but become similar after tissue distribution.
Approximately 80–95% of circulating doxycycline is bound to plasma proteins.
The biological half-life ranges from 12 to 24 hours.
Doxycycline is more lipid-soluble than tetracycline and is widely distributed throughout body tissues and fluids.
In patients with normal renal function, approximately 40% of a dose is excreted slowly in the urine, while the majority is eliminated in the faeces following intestinal chelation.
Although urinary excretion decreases in patients with renal impairment, increased faecal elimination compensates, and significant accumulation generally does not occur. Removal by haemodialysis is negligible.
INDICATIONS
Doxycycline is indicated for infections caused by susceptible organisms, including:
Respiratory tract infections
Sinusitis
Pharyngitis
Pneumonia caused by Mycoplasma or Legionella
Psittacosis
Genitourinary infections
Non-specific urethritis
Lymphogranuloma venereum
Granuloma inguinale
Gonorrhoea
Gonococcal salpingitis
Epididymitis
Acute epididymo-orchitis
Endocervical infections
Syphilis
Ophthalmic infections
Trachoma
Inclusion conjunctivitis
Intestinal infections
Cholera
Whipple's disease
Tropical sprue
Malaria
Short-term prophylaxis of malaria caused by Plasmodium falciparum in short-term travellers.
Miscellaneous infections
Rickettsial infections
Brucellosis
Tularemia
Actinomycosis
Lyme disease
Yaws
Relapsing fever
CONTRAINDICATIONS
Do not use Doxycycline if:
You are allergic to doxycycline or any other tetracycline antibiotic.
You have systemic lupus erythematosus.
You are receiving antacid therapy or consuming large amounts of milk or calcium-containing products without appropriate spacing.
You are taking potentially hepatotoxic medicines unless advised by your doctor.
WARNINGS
Do not use concomitantly with hepatotoxic medicines.
Raised intracranial pressure may occur, particularly in infants and in patients receiving vitamin A or retinoids.
Doxycycline may interfere with laboratory tests, including urinary catecholamine and glucose determinations.
Use with caution in patients with liver impairment.
Elderly and frail patients are more susceptible to the hepatotoxic and anti-anabolic effects of doxycycline.
Symptoms of myasthenia gravis may worsen during treatment.
DOSAGE AND DIRECTIONS FOR USE
Doxycycline is usually administered once daily.
Capsules should be taken with plenty of water while sitting or standing to reduce the risk of oesophageal irritation or ulceration.
It may be taken one hour before or two hours after meals.
Adults
Day 1
200 mg daily (either as a single dose or divided into two 100 mg doses)
Maintenance
100 mg once daily
For severe infections, 200 mg daily may be continued throughout treatment, as directed by the physician.
Children
Use in children should follow current clinical guidelines.
Doxycycline is generally not recommended in children younger than 8 years, except where the expected benefit outweighs the risk.
SIDE EFFECTS AND SPECIAL PRECAUTIONS
Common side effects include:
Nausea
Vomiting
Diarrhoea
Abdominal discomfort
Other reported effects include:
Dry mouth
Glossitis
Stomatitis
Difficulty swallowing
Oesophageal ulceration (especially when taken without sufficient water or immediately before lying down)
Enterocolitis
Raised intracranial pressure (which may present with headache or bulging fontanelle in infants)
Increased blood urea due to anti-anabolic effects
Hypersensitivity reactions may include:
Skin rash
Urticaria
Maculopapular rash
Erythema
Exfoliative dermatitis
Angioedema
Fixed drug eruption
Toxic epidermal necrolysis
Drug fever
Asthma
Anaphylaxis
Patients should avoid excessive exposure to sunlight or ultraviolet light because photosensitivity reactions may occur.
Use with caution in patients with impaired liver function.
Symptoms of myasthenia gravis may worsen during treatment.
Doxycycline should generally not be administered together with penicillin because the bacteriostatic action of doxycycline may interfere with the bactericidal action of penicillin.
INTERACTIONS
The absorption of doxycycline is reduced by products containing:
Aluminium
Bismuth
Calcium
Iron
Magnesium
Zinc
These include:
Antacids
Sucralfate
Iron supplements
Milk and dairy products
Mineral supplements
These products should be taken several hours apart from doxycycline.
Penicillin should generally not be administered concomitantly because antagonism may occur.
PREGNANCY AND LACTATION
Doxycycline should not be used during pregnancy.
It crosses the placenta and may be deposited in developing bones and teeth.
Use during pregnancy may cause:
Permanent tooth discoloration
Impaired bone growth
Severe maternal liver toxicity
Doxycycline is also excreted in breast milk and should generally not be used during breastfeeding.
Consult your doctor or pharmacist before taking this medicine if you are pregnant or breastfeeding.
OVERDOSAGE
In the event of overdose:
Discontinue treatment.
Provide supportive and symptomatic treatment.
Haemodialysis does not significantly remove doxycycline.
IDENTIFICATION
Green/green hard gelatin capsules containing a white powder.
PRESENTATION
Blister packs containing 10 capsules.
INACTIVE INGREDIENTS
Lactose
Cabosil
Magnesium Stearate
Sodium Lauryl Sulphate
STORAGE INSTRUCTIONS
Store below 30°C in a cool, dry place.
Protect from light and moisture.
Keep out of the reach of children.
Date of Publication: January 2015
Manufactured by:
Letap Pharmaceuticals Ltd.
P.O. Box 3346
Accra, Ghana