Tecovirimat
Indications
Tecovirimat is used for:
Human Smallpox Disease
Adult Dose
Human Smallpox Disease
Antiviral agent indicated for treatment of human smallpox disease caused by variola virus
>40 kg: 600 mg PO BID for 14 days
Hepatic impairment
Mild, moderate, or severe (Child-Pugh class A, B, or C): No dosage adjustment required
Child Dose
Human Smallpox Disease
Indicated for treatment of human smallpox disease caused by variola virus in adults and children weighing ?13 kg
<13 kg: Safety and efficacy not established
13 kg to <25 kg: 200 mg PO BID for 14 days
25 kg to <40 kg: 400 mg PO BID for 14 days
>40 kg: 600 mg PO BID for 14 days
Renal Dose
Renal impairment
Mild, moderate, severe, or patients with ESRD requiring hemodialysis: No dosage adjustment required
Administration
Administer within 30 minutes after a full meal of moderate or high fat
Contra Indications
Precautions
Coadministration with repaglinide (an antidiabetic agent) may cause mild-to-moderate hypoglycemia; monitor blood glucose and monitor for hypoglycemic symptoms when administering tecovirimat with repaglinide (see Drug interaction overview)
Pregnancy-Lactation
Pregnancy
There are no available data regarding use in pregnant women
Animal studies
In animal reproduction studies, no embryofetal developmental toxicity was observed in mice and rabbits during the period of organogenesis at tecovirimat exposures (AUC) up to 23 and 24 times higher than human exposure at the recommended human dose
Infertility
No data are available regarding the effect on female and male reproductive potential in humans
Decreased fertility due to testicular toxicity was observed in male mice
Lactation
The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child or from the underlying maternal condition
Interactions
Vaccines
No vaccine-drug interaction studies have been performed in humans
Some animal studies have indicated that coadministration of tecovirimat at the same time as live smallpox vaccine (vaccinia virus) may reduce the immune response to the vaccine
The clinical impact of this interaction on vaccine efficacy is unknown
Adverse Effects
Side effects of Tecovirimat :
>10%
Headache (12%)
1-10%
Nausea (5%)
Abdominal pain (2%)
Vomiting (2%)
<2%
Gastrointestinal: Dry mouth, chapped lips, dyspepsia, eructation, oral paresthesia
General and administration site: Pyrexia, pain, chills, malaise, thirst
Investigations: Abnormal electroencephalogram, hematocrit decreased, hemoglobin decreased, heart rate increased
Musculoskeletal and connective tissue: Arthralgia, osteoarthritis
Nervous system: Migraine, disturbance in attention, dysgeusia, paresthesia
Psychiatric: Depression, dysphoria, irritability, panic attack
Respiratory, thoracic, and mediastinal disorders: Oropharyngeal pain
Skin and subcutaneous tissue: Palpable purpura, rash, pruritic rash, facial redness, facial swelling, pruritus
Mechanism of Action
Antiviral agent; targets and inhibits the activity of the orthopoxvirus VP37 protein (encoded by and highly conserved in all members of the orthopoxvirus genus) and blocks its interaction with cellular Rab9 GTPase and TIP47, which prevents the formation of egress-competent enveloped virions necessary for cell-to-cell and long-range dissemination of virus