Lippincott ^® NursingCenter ^®

gepirone

Exxua

Pharmaceutical company: Fabre-Kramer Pharmaceuticals

Pharmacologic classification: 5HT1A receptor agonist

Therapeutic classification: Antidepressant
 

AVAILABLE FORMS

Tablets (extended-release): 18.2 mg, 36.3 mg, 54.5 mg, 72.6 mg
 

INDICATIONS AND DOSAGES

Major depressive disorder

Adults: Start at 18.2 mg PO once daily. May increase to 36.3 mg once daily on day 4, 54.5 mg once daily after day 7, and 72.6 mg once daily after day 14 based on clinical response and tolerability. Maximum daily dose is 72.6 mg.
 

Adjust-a-dose: In older adults, patients with creatinine clearance less than 50 mL/minute or Child-Pugh class B liver impairment, maximum dosage is 36.3 mg once daily after day 7. In patients also receiving a moderate CYP3A4 inhibitor, reduce gepirone dosage by 50%.

CONTRAINDICATIONS AND CAUTIONS

• Boxed Warning: There is an increased risk of suicidal thinking and behavior in children and young adults taking antidepressants. Closely monitor for worsening and emergence of suicidal thoughts and behaviors. This drug isn't approved for use in pediatric patients.
• Contraindicated in patients with hypersensitivity to gepirone or its components, patients with prolonged QTc interval greater than 450 msec at baseline, congenital long QT syndrome, or Child-Pugh class C liver impairment.
• This drug isn't approved for use in treating bipolar depression.
• This drug may precipitate a manic, mixed, or hypomanic episode, especially in patients with bipolar disorder or who have risk factors for bipolar disorder (family history of bipolar disorder, suicide, or depression).
• Dialyzable drug: Unknown.

PREGNANCY-LACTATION-REPRODUCTION

• Studies during pregnancy are inadequate. Health care providers are encouraged to register patients in the National Pregnancy Registry for Antidepressants at 1-866-961-2388 or https://womensmentalhealth.org/research/pregnancyregistry/antidepressants/.
• Consider the risk of untreated depression during pregnancy and postpartum with the risk of complications to the newborn upon delivery.
• Neonates exposed to serotonergic antidepressants in the third trimester may experience complications upon delivery, including respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremors, jitteriness, irritability, and constant crying that require prolonged hospitalization, respiratory support, and tube feeding. Exposure during late pregnancy may also increase the risk of persistent pulmonary hypertension, which is associated with substantial neonatal morbidity and mortality.
• There are no data on the presence of gepirone in human milk, the effects on the breastfed infant, or the effects on milk production. Use cautiously during breastfeeding and monitor for infant irritability, restlessness, excessive somnolence, decreased feeding, and weight loss.

INTERACTIONS

Drug-drug. CYP3A4 inducers (bosentan, phenytoin): May significantly decrease gepirone level. Avoid use together.
Drugs that prolong the QTc interval (amiodarone, haloperidol, ciprofloxacin, methadone, amitriptyline): May increase QTc prolonging effects of gepirone and the risk of cardiac arrhythmias. Monitor patients with ECGs more frequently.
MAO inhibitors (selegiline, phenelzine, linezolid, IV methylene blue): Increase the risk of serotonin syndrome. Use together or within 14 days is contraindicated.
Moderate CYP3A4 inhibitors (erythromycin, diltiazem): May increase gepirone level. If use can't be avoided, reduce gepirone dosage by 50%.
Serotonergic drugs (SSRIs, tricyclic antidepressants): May increase the risk of serotonin syndrome. If serotonin syndrome occurs, consider discontinuation of gepirone or concomitant serotonergic drugs.
Strong CYP3A4 inhibitors (clarithromycin, indinavir, ketoconazole): May increase gepirone level. Use together is contraindicated.
Drug-herb. St. John's wort: May decrease gepirone level. Discourage use together.
 

ADVERSE REACTIONS

CNS: dizziness, lightheadedness, headache, fatigue, sedation, somnolence, insomnia, paresthesia, agitation, feeling jittery, lethargy, confusion, increased energy, feeling abnormal, hypoesthesia, poor quality sleep, thinking abnormalities.
CV: palpitations, increased heart rate, peripheral edema.
EENT: dry mouth, nasal congestion, nasopharyngitis.
GI: nausea, diarrhea, vomiting, abdominal pain, dyspepsia, increased appetite, constipation.
Metabolic: weight gain.
Respiratory: upper respiratory infection, dyspnea.
Skin: hyperhidrosis.
Other: breast tenderness.

Reactions in bold italics are life-threatening.
 

Released: December 2023

Nursing Drug Handbook

© 2023 Wolters Kluwer

---

motixafortide

palovarotene

Sohonos

Pharmaceutical company: IPSEN Biopharmaceuticals, Inc.

Pharmacologic classification: Retinoic acid receptor agonist

Therapeutic classification: Metabolic agent
 

AVAILABLE FORMS

Capsules: 1 mg, 1.5 mg, 2.5 mg, 5 mg, 10 mg
 

INDICATIONS AND DOSAGES

Reduction in the volume of new heterotopic ossification in patients with fibrodysplasia ossificans progressiva (FOP)

Adults and children age 14 and older: Daily dosing regimen: 5 mg PO daily. Stop daily dosing when flare-up dosing begins. Flare-up dosing is 20 mg PO daily for 4 weeks, followed by 10 mg PO daily for 8 weeks (for a total of 12 weeks), even if symptoms resolve earlier, then return to daily dosing of 5 mg.
Children ages 8 to 13 (females) and ages 10 to 13 (males) weighing 60 kg or more: Follow adult dosing.
Children ages 8 to 13 (females) and ages 10 to 13 (males) weighing 40 to 59.9 kg: Daily dosing: 4 mg PO daily. Flare-up dosing: 15 mg PO daily weeks 1 to 4, then 7.5 mg PO daily weeks 5 to 12.
Children ages 8 to 13 (females) and ages 10 to 13 (males) weighing 20 to 39.9 kg: 3 mg PO daily. Flare-up dosing: 12.5 mg PO daily weeks 1 to 4, then 6 mg PO daily weeks 5 to 12.
Children ages 8 to 13 (females) and ages 10 to 13 (males) weighing 10 to 19.9 kg: 25 mg PO daily. Flare-up dosing: 10 mg PO daily weeks 1 to 4, then 5 mg PO daily weeks 5 to 12.

Adjust-a-dose: Administer the initial flare-up dosage once daily for 4 weeks, then administer the lower flare-up dosage once daily for 8 weeks (for a total of 12 weeks of flare-up treatment), even if symptoms resolve earlier, then return to daily dosing. If, during flare-up treatment, the patient experiences marked worsening of the original flare-up site or another flare-up at a new location, restart the 12-week flare-up dosing with the week 1 to 4 dose. For flare-up symptoms that have not resolved at the end of the 12-week period, the week 5 to 12 flare-up dose may be extended in 4-week intervals and continued until the flare-up symptoms resolve. If new flare-up symptoms occur after daily dosing is resumed, flare-up dosing may be restarted.

If the patient requires dosage reduction for adverse reactions during either daily dosing or flare-up dosing, refer to the manufacturer's instructions. May reduce dosage further or discontinue temporarily or permanently if adverse reactions don't improve. Subsequent flare-up dosing should be initiated at the last previously tolerated dose. If concomitant use with moderate CYP3A inhibitors is necessary, reduce palovarotene dose by half; see manufacturer's instructions for specifics.
 

CONTRAINDICATIONS AND CAUTIONS

• Contraindicated in patients hypersensitive to retinoids, or to any component of this drug.
• Boxed Warning: Premature epiphyseal closure occurs in growing pediatric patients treated with this drug. Close monitoring is recommended.
• Mucocutaneous adverse reactions, including dry skin, dry lips, pruritis, rash, alopecia, erythema, skin exfoliation, photosensitivity reactions, and dry eye have occurred. This may increase the risk of skin and soft tissue infections, particularly paronychia and decubitus ulcer. Dosage reduction may be required.
• May increase bone toxicity, including reductions in bone mass and spontaneous osteoporosis and fracture. Bone spurs and calcification of tendons or ligaments may also occur, especially with long-term use at high doses.
• May increase the risk of decreased vertebral bone mineral content and bone density, and vertebral fractures (T4 to L4).
• Depression, anxiety, mood alterations and suicidal thoughts and behaviors may occur.
• Night blindness may occur and make driving at night hazardous.
• The safety and effectiveness for the treatment of FOP have not been established in female children younger than age 8 or male children younger than age 10.
• This drug isn't recommended for use in patients with Child-Pugh class B or C liver impairment, or those with creatinine clearance 15 to 29 mL/min.
• Dialyzable drug: Unknown.

 

PREGNANCY-LACTATION-REPRODUCTION

• Boxed Warning: This drug may cause fetal harm and is contraindicated during pregnancy. Because of the risk of teratogenicity and to minimize fetal exposure, this drug is to be administered only if conditions for pregnancy prevention are met.
• Negative serum pregnancy test required at least 1 week prior to initiating therapy, periodically during treatment, and one month after treatment discontinuation.
• Females of reproductive potential must use an effective method of contraception at least 1 month prior to treatment, during treatment, and for 1 month after the last dose.
• If pregnancy occurs during treatment, discontinue the drug immediately and refer the patient to an obstetrician/gynecologist experienced in reproductive toxicity.
• It's unknown if this drug crosses into human milk. Breastfeeding isn't recommended during treatment and for at least 1 month after the last dose.
• Palovarotene is present in semen, but at levels unlikely to affect fetal development.

 

INTERACTIONS

Drug-drug. Strong or moderate CYP3A4 inhibitors (ketoconazole, erythromycin): May increase palovarotene concentrations. Avoid use together. If moderate inhibitors are used, reduce palovarotene dose by 50%.
Strong or moderate CYP3A4 inducers (rifampicin): May decrease palovarotene concentrations. Avoid use together.
Tetracyclines: May increase risk of benign intracranial hypertension. Avoid use together.
Vitamin A: May cause additive effects and risk of hypervitaminosis A. Avoid use together.
Drug-food. Grapefruit, pomelo, or juices containing these fruits: May increase palovarotene levels. Don't use together.
Drug-lifestyle. Sun exposure: May increase risk of mucocutaneous adverse reactions and photosensitivity. Avoid excessive sun exposure or artificial UV light. Sunscreen, protective clothing, and sunglasses should be used when exposure is unavoidable.
 

ADVERSE REACTIONS

CNS: headache, migraine, fatigue.
CV: peripheral edema.
EENT: dry eye.
GI: nausea.
Hepatic: increased ALT levels.
Metabolic: hypertriglyceridemia.
Musculoskeletal: premature epiphyseal closure, arthralgia, extremity pain, back pain, musculoskeletal pain, myalgia.
Skin: dry skin, dry lips, pruritus, rash, alopecia, erythema, skin peeling.
Other: hypersensitivity.

 

Reactions in bold italics are life-threatening.
 

Released: December 2023

Nursing Drug Handbook

© 2023 Wolters Kluwer

Download these updates as a PDF