AfyaIndex — Drug Search

01 Risk first

Safety essentials

The information most likely to change a prescribing or dispensing decision.

Contraindications

CONTRAINDICATIONS Ketoconazole shampoo, 2% is contraindicated in persons who have known hypersensitivity to the active ingredient or excipients of this formulation.

Precautions

PRECAUTIONS Severe hypersensitivity reactions, including anaphylaxis, have been reported during post-marketing use of ketoconazole shampoo.
If a reaction suggesting sensitivity or chemical irritation should occur, use of the medication should be discontinued.
INFORMATION FOR PATIENTS Patients should be advised of the following: Ketoconazole shampoo, 2% may be irritating to mucous membranes of the eyes and contact with this area should be avoided.
The following have been reported with the use of ketoconazole shampoo, 2%: hair discoloration and abnormal hair texture, removal of the curl from permanently waved hair, itching, skin burning sensation and contact dermatitis, hypersensitivity, angioedema, alopecia, rash, urticaria, skin irritation, dry skin, and application site reactions.
Patients who develop allergic reactions, such as generalized rash, skin reactions, severe swelling, angioedema, or shortness of breath should discontinue ketoconazole shampoo, 2% and contact their physician immediately.
CARCINOGENESIS & MUTAGENESIS & IMPAIRMENT OF FERTILITY Long-term studies to assess the carcinogenic potential of ketoconazole shampoo, 2% have not been conducted.
A long-term feeding study of ketoconazole in Swiss Albino mice and in Wistar rats showed no evidence of oncogenic activity.
The dominant lethal mutation test in male and female mice revealed that single oral doses of ketoconazole as high as 80 mg/kg were not genotoxic.
The Ames Salmonella microsomal activator assay was also negative.
PREGNANCY Teratogenic effects: Pregnancy Category C: There are no adequate and well-controlled studies in pregnant women.
Ketoconazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
In humans, ketoconazole is not detected in plasma after chronic shampooing on the scalp.

02 Point of care

Dosing matrix

Population and organ-function guidance, shown together for faster comparison.

Adult

DOSAGE & ADMINISTRATION Apply the shampoo to the damp skin of the affected area and a wide margin surrounding this area. Lather, leave in place for 5 minutes, and then rinse off with water. One application of the shampoo should be sufficient.

Paediatric

PEDIATRIC USE Safety and effectiveness in children have not been established.

Renal

Fluconazole dose-adjust in CKD; amphotericin nephrotoxicity high-alert.

CrCl 0–120: Confirm renal dosing in product SmPC / primary label.

Hepatic

Monitor LFTs for courses >14 days or higher-risk patients.

03 Clinical use

Use, effects & interactions

Indications

INDICATIONS & USAGE Ketoconazole shampoo, 2% is indicated for the treatment of tinea (pityriasis) versicolor caused by or presumed to be caused by Pityrosporum orbiculare (also known as Malassezia furfur or M. orbiculare ) .
Note: Tinea (pityriasis) versicolor may give rise to hyperpigmented or hypopigmented patches on the trunk which may extend to the neck, arms and upper thighs.
Treatment of the infection may not immediately result in normalization of pigment to the affected sites.
Normalization of pigment following successful therapy is variable and may take months, depending on individual skin type and incidental sun exposure.
Although tinea versicolor is not contagious, it may recur because the organism that causes the disease is part of the normal skin flora.

Adverse effects

ADVERSE REACTIONS Clinical Trials Experience In 11 double-blind trials in 264 patients using ketoconazole shampoo, 2% for the treatment of dandruff or seborrheic dermatitis, an increase in normal hair loss and irritation occurred in less than 1% of patients.
In three open label safety trials in which 41 patients shampooed 4-10 times weekly for six months, the following adverse experiences each occurred once: abnormal hair texture, scalp pustules, mild dryness of the skin, and itching.
As with other shampoos, oiliness and dryness of hair and scalp have been reported.
In a double-blind, placebo-controlled trial in which patients with tinea versicolor were treated with either a single application of ketoconazole shampoo, 2% (n=106), a daily application for three consecutive days (n=107), or placebo (n=105), drug-related adverse events occurred in 5 (5%), 7 (7%) and 4 (4%) of patients, respectively.
The only events that occurred in more than one patient in any one of the three treatment groups were pruritus, application site reaction, and dry skin
none of these events occurred in more than 3% of the patients in any one of the three groups.
Post-marketing Experience Because these reactions are reported voluntarily from a population of uncertain size, it is not possible to reliably estimate their frequency.
The following adverse drug reactions have been identified during post-marketing experience with ketoconazole shampoo: there have been reports of hair discoloration and abnormal hair texture, itching, skin burning sensation, contact dermatitis, hypersensitivity, angioedema, alopecia, rash, urticaria, skin irritation, dry skin, and application site reactions.

Drug interactions

Open multi-drug checker ↗

Match agent to site and species.
For tinea, continue topical beyond clearance.
Invasive fungal disease needs ID/specialist input and source control.

04 Pharmacology

Mechanism & disposition

Azoles inhibit fungal CYP51 (lanosterol 14α-demethylase), depleting ergosterol and disrupting membrane integrity.

Azoles inhibit fungal CYP51 (lanosterol 14…Terbinafine inhibits squalene epoxidase.Polyenes bind ergosterol creating membrane…

Read complete mechanism

Azoles inhibit fungal CYP51 (lanosterol 14α-demethylase), depleting ergosterol and disrupting membrane integrity. Terbinafine inhibits squalene epoxidase. Polyenes bind ergosterol creating membrane pores. Echinocandins inhibit β-glucan synthase (cell wall).

Onset

Days for clinical response (varies)

Duration

Days–weeks per indication

Route

ORAL / TOPICAL / IV

05 Special populations

Pregnancy, lactation & diet

Pregnancy

PREGNANCY Teratogenic effects: Pregnancy Category C: There are no adequate and well-controlled studies in pregnant women. Ketoconazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. In humans, ketoconazole is not detected in plasma after chronic shampooing on the scalp. Ketoconazole has been shown to be teratogenic (syndactylia and oligodactylia) in the rat when given orally in the diet at 80 mg/kg/day (a dose 10 times the maximum recommended human oral dose). However, these effects may be related to maternal toxicity, which was seen at this and higher dose levels.

Lactation

NURSING MOTHERS There are no adequate and well-controlled studies in nursing women. Ketoconazole is not detected in plasma after chronic shampooing on the scalp. Caution should be exercised when ketoconazole shampoo, 2% is administered to a nursing woman.

06 Kenya market

Brands & loaded prices

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Ketoconazole, topical