Ketotifen

R06A - Antihistamines for systemic use ATC R06AX17 Small molecule approved 1999 Topical Prodrug Natural product

Active form: Norketotifen.

JFDA label: Tefanyl tablet

Indications

Approved

Eye Manifestations — eye allergy
Hypersensitivity — allergic disease

Off-label

Conjunctivitis, Allergic
Contracture
Dyspepsia
Fibromyalgia
Peanut Hypersensitivity
Peripheral Nervous System Diseases
Rhinitis, Allergic, Perennial
Severe Acute Respiratory Syndrome

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Vascular disorders (1)

Not Known Hypertension

Nervous system disorders (6)

Not Known Dizziness · Headache · Loss of consciousness · Paraesthesia · Somnolence · Syncope

Hepatobiliary disorders (2)

Not Known Hepatic enzyme increased · Hepatitis

Blood and lymphatic system disorders (1)

Not Known Thrombocytopenia

Gastrointestinal disorders (7)

Not Known Abdominal pain · Diarrhoea · Dry mouth · Gastrointestinal pain · Increased appetite · Nausea · Vomiting

Skin and subcutaneous tissue disorders (6)

Not Known Dermatitis · Erythema multiforme · Pruritus · Rash · Stevens-Johnson syndrome · Urticaria

Psychiatric disorders (3)

Not Known Insomnia · Irritability · Sleep disorder

Eye disorders (3)

Not Known Dry eye · Eyelid disorder · Eyelid oedema

Infections and infestations (2)

Not Known Cystitis noninfective · Infection

Investigations (2)

Not Known Body temperature increased · Weight increased

General disorders and administration site conditions (8)

Not Known Bladder pain · Conjunctival hyperaemia · Cystitis · Haematochezia · Nervousness · Pain · Shock · Tension

Respiratory, thoracic and mediastinal disorders (1)

Not Known Epistaxis

Dosing

Source: openFDA

Directions ▪ adults and children 3 years and older: ▪ put 1 drop in the affected eye(s) twice daily, every 8-12 hours, no more than twice per day ▪ if using other ophthalmic products while using this product, wait at least 5 minutes between each product ▪ children under 3 years of age: consult a doctor

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Warnings For external use only Do not use ▪ if you are sensitive to any ingredient in this product ▪ if solution changes color or becomes cloudy ▪ to treat contact lens related irritation When using this product ▪ remove contact lenses before use ▪ wait at least 10 minutes before re-inserting contact lenses after use ▪ do not touch tip of container to any surface to avoid contamination ▪ replace cap after each use

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

Because absorption from the eye is limited, ketotifen would not be expected to cause any adverse

Chemistry & Properties

Formula	C19H19NOS
Molecular weight	309.43 g/mol
IUPAC name	2-(1-methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-8-one
CAS	34580-13-7
PubChem CID	3827
InChIKey	`ZCVMWBYGMWKGHF-UHFFFAOYSA-N`
logP	4.01 (XLogP 3.2)
Polar surface area	20.31 Å²
H-bond acceptors / donors	3 / 0
Drug-likeness (QED)	0.73
Lipinski violations	0

SMILES

CN1CCC(=C2c3ccccc3CC(=O)c3sccc32)CC1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes

Enzyme interactions

Enzyme	Role	Detail
CYP2B6	Inhibitor	—
CYP2C19	Substrate	—
CYP2D6	Inhibitor	—

Receptor binding (top 2)

Target	Action	Affinity
H1	Binding	pKi 10.4
H1 receptor (HRH1)	Antagonist	pKi 8.6

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (10)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Orchazid Eye Drops	Ophthalmic Solution 0.345 mg/ml	5 ml	Nabulsi Drug Store	2.860
Ketonil-	Tablet 1 mg	30 tab	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	3.500
Profilar Tablets	Tablet 1 mg	30 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	3.500
Tefanyl tablet	Tablet 1 mg	30 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	3.500
Tefanyl syrup	Syrup 1 mg/5 ml	100 ml	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	3.850
ketonil syrup	Syrup 1 mg/5 ml	100 ml	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	4.500
Apizad	Solution 0.025 %	5 ml	Amman Pharmaceutical Indusries	4.830
Profilar Syrup	Syrup 1 mg/5 ml	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	4.900
Profilar Tablets	Tablet 1 mg	1000 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	93.330
Tefanyl tablet	Tablet 1 mg	1005 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	93.800