DRUG

MONOGRAPHS

:Done By
 Shahad Mohammed AL-rebie
 Shatha marzoq AL-sofyani
 Wjood Ahmed AL-thomali
 Deema Ebad AL-qurashi
 Waad Mohammad AL-amri
ONDANSETRON( Zofran® , Zuplenz® )

Drug classification Supplied

-Antiemetic • Generic
-Seretonin Receptor Antagonist, 5-HT3 ◦ Oral Tablet, Disintegrating: 4 MG, 8 MG
• Zuplenz
◦ Oral Film: 4 MG, 8 MG

Mechanism of Action Metabolism

Ondansetron is a selective 5-hydroxytryptamine-3 (5-HT3)- • Hepatic: Extensive via hydroxylation followed by glucuronide or sulfate
receptor antagonist used for the prevention of chemotherapy- conjugation
induced nausea and vomiting. Ondansetron may work by blocking • Substrate of CYP3A4, CYP1A2, and CYP2D6
5-HT3 receptors peripherally on vagal nerve terminals and
centrally in the chemoreceptor trigger zone. Onset
• Tmax, Oral soluble film: 1.3 hours
• Tmax, Oral disintegrating tablets: 1.17 hours

Elimination Half Life

• 4.6 hours, oral soluble film; 4.79 hours, oral disintegrating tablets
• Hepatic impairment: 11.6 to 20 hours

Indications Percautions
FDA-Labeled Indications • Cardiovascular: Myocardial ischemia and QT prolongation and potentially
• Chemotherapy-induced nausea and vomiting, Highly fatal torsade de pointes, has been reported; monitoring recommended in
emetogenic chemotherapy; Prophylaxis patients with electrolyte abnormalities (eg, hypokalemia, hypomagnesemia),
• Chemotherapy-induced nausea and vomiting, Moderately bradyarrhythmias, congestive heart failure, and with concomitant use of
emetogenic chemotherapy; Prophylaxis medications that proloong QT interval
• Postoperative nausea and vomiting; Prophylaxis • Cardiovascular: Congenital long QT syndrome; avoid use
• Radiation-induced nausea and vomiting; Prophylaxis • Endocrine and Metabolic: Use caution in phenylketonurics; contains
phenylalanine
• Gastrointestinal: Use caution following abdominal surgery or
Non-FDA Labeled Indications chemotherapy-induced nausea and vomiting as it may mask a progressive
Gastroenteritis - Vomiting ileus, gastric distention, or both; monitoring recommended.
• Immunologic: Hypersensitivity reactions, including anaphylaxis and
bronchospasm,
• Serotonin syndrome: Serotonin syndrome, sometimes fatal, has been
reported, particularly with the concomitant use of serotonergic medications
and occurred in a post-anesthesia care unit or an infusion center; monitoring
required and discontinue use if suspected

Side Effects Contraindications

May include constipation, diarrhea, headache, fatigue, or • Concomitant use of apomorphine
malaise. • Hypersensitivity to ondansetron or any component of the product
• Instruct patient on how to take the oral soluble films.

Adult dose Pediatric dose

Chemotherapy-induced nausea and vomiting, Highly emetogenic • Chemotherapy-induced nausea and vomiting, Moderately emetogenic
chemotherapy; Prophylaxis chemotherapy; Prophylaxis
◦ 24 mg dissolved orally on tongue 30 minutes prior to the start of ◦ (4 to 11 years) 4 mg dissolved orally on tongue 30 minutes prior to
a single-day chemotherapy chemotherapy, repeated 4 and 8 hours after the first dose, then every 8 hours
for 1 to 2 days post chemotherapy
◦ (12 years or older) 8 mg dissolved orally on tongue 30 minutes prior to
Chemotherapy-induced nausea and vomiting, Moderately chemotherapy and repeated in 8 hours, then 8 mg every 12 hours for 1 to 2
emetogenic chemotherapy; Prophylaxis days post chemotherapy
◦ 8 mg dissolved orally on tongue 30 minutes prior to • Gastroenteritis - Vomiting
chemotherapy and repeated in 8 hours, then 8 mg every 12 hours ◦ (Orally disintegrating tablet, 8 to 15 kg) 2 mg dissolved orally as a single
for 1 to 2 days post chemotherapy dose (study dose);
◦ (Orally disintegrating tablet, 15 to 30 kg) 4 mg dissolved orally as a single
Postoperative nausea and vomiting; Prophylaxis dose (study dose)
◦ 16 mg dissolved orally on the tongue 1 hour before anesthesia ◦ (Orally disintegrating tablet, greater than 30 kg) 8 mg dissolved orally as a
induction single dose (study dose)
Radiation-induced nausea and vomiting; Prophylaxis
◦ Daily fractionated radiotherapy to abdomen: 8 mg dissolved
orally on tongue 1 to 2 hours prior to radiotherapy and every 8
hours after first dose for each day radiotherapy is given
ESKETAMINE (Spravato®)

Drug classification Supplied

-Antidepressant Spravato * Nasal Spray: 28 MG/0.2 ML
-N-Methyl-D-Aspartate Receptor Antagonist

Mechanism of Action Metabolism

Esketamine, is the S-enantiomer of racemic ketamine. Ketamine • Liver: Extensive
hydrochloride is a strong non-selective, non-competitive • Substrate of CYP3A4, CYP2B6, CYP2C9, CYP2C19
antagonist of the N-methyl-D-aspartate (NMDA) receptor, with • Noresketamine (major): Active
additional effects as an indirect and direct alpha-amino-3-
hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor
Onset
agonist, hyperpolarization-activated cyclic nucleotide-gated
•Tmax, intranasal: 20 to 40 minutes
(HCN) channel antagonist, mu-, kappa- and delta-opioid receptor
agonist, serotonin receptor 5-HT 2 agonist, dopamine 2 receptor
Elimination Half Life
agonist, and antiinflammatory. Ketamine's main effects on
•7 to 12 hours
depression and pain rely heavily on indirect activation of AMPA
receptors.

Indications Percautions
FDA-Labeled Indications •Abuse: Increased risk of abuse and misuse in patients with a history of drug
 Major depressive disorder, Depressive symptoms in patients abuse or dependence; monitoring recommended
with acute suicidal ideation or behavior; Adjunct.  Cardiovascular: Increase in blood pressure has been reported at all
 Major depressive disorder, Treatment-resistant; Adjunct. recommended doses; monitoring recommended especially in patients with
history of hypertensive encephalopathy due to increased risk for developing
encephalopathy
 Neurologic: Short-term cognitive impairment has been reported; instruct
patients to avoid potentially hazardous activities requiring complete mental
alertness and motor coordination (eg, driving a motor vehicle or operating
machinery) until the next day following a restful sleep
 Renal: Lower urinary tract symptoms (eg, pollakiuria, dysuria, micturition
urgency, nocturia, and cystitis) have been reported; monitoring
recommended
 Reproductive: May cause fetal harm; advise women of reproductive
potential to consider pregnancy planning and prevention

Side Effects Contraindications

May include dissociation, dizziness, nausea, sedation, vertigo,  Aneurysmal vascular disease (including thoracic and abdominal aorta,
hypoesthesia, anxiety, lethargy, increased blood pressure, intracranial, and peripheral arterial vessels) or arteriovenous
vomiting, and feeling drunk. malformation.
 History of intracerebral hemorrhage.
 Hypersensitivity to esketamine, ketamine, or any component of the
product.

Adult dose Pediatric dose

 Major depressive disorder, Depressive symptoms in patients • The safety and effectiveness in pediatric patients have not been established.
with acute suicidal ideation or behavior; Adjunct
* 84 mg intranasally twice weekly for 4 weeks in combination
with an oral antidepressant; dosage may be reduced to 56 mg
twice per week based upon tolerability; evaluate therapeutic
benefit to determine need for continued treatment after 4 weeks,
use beyond 4 weeks has not been systematically evaluated.
 Major depressive disorder, Treatment-resistant; Adjunct
* Induction, 56 mg intranasally on day 1, then 56 or 84 mg
twice a week during weeks 1 through 4 based on efficacy and
tolerability; give with an oral antidepressant
* Maintenance, 56 or 84 mg intranasally once a week during
weeks 5 through 8, then 56 or 84 mg every 2 weeks or once a
week during week 9 and thereafter; individualize frequency with
the least frequent dosing to maintain remission/response; give
with an oral antidepressant.
 EXEMESTANE (Aromasin®)

Drug classification Supplied

• Antineoplastic Agent • Generic
• Aromatase Inhibitor ◦ Oral Tablet: 25 MG
• Aromasin
◦ Oral Tablet: 25 MG

Mechanism of Action Metabolism

The principle source of circulating estrogen in postmenopausal Systemic: Hepatic: extensively via CYP3A4 pathway; Active Metabolite: 17-
women comes from conversion of androstenedione and dihydro metabolite
testosterone (synthesized in the adrenals and ovaries) to estrone
and estradiol via the aromatase enzyme. Exemestane acts as a Excretion
false substrate for the aromatase enzyme, causing an irreversible Systemic: Fecal: 42%; Renal: 42%; < 1% unchanged
inhibition. This inhibition results in estrogen deprivation to
hormone dependent breast cancer cells. Exemestane has no effect Elimination Half Life
on other steroidogenic pathway enzymes. Exemestane has not Systemic: 24 h
been shown to affect cortisol or aldosterone secretion. At daily
doses of 200 mg or greater, increases in testosterone and
androstenedione levels were observed. Slight, non-dose-
dependent increases in serum luteinizing hormone (LH) and
follicle-stimulating hormone (FSH) were observed at low doses.
A dose-dependent decrease in sex hormone binding globulin
(SHBG) was observed at daily doses of 2.5 mg or greater.

Indications Precautions
FDA-Labeled Indications • Concomitant use: Do not give with estrogen-containing products
• Breast cancer, Adjuvant, postmenopausal, estrogen receptor- • Endocrine and metabolic: Vitamin D deficiency may occur due to increased
positive, following 2 to 3 years of adjuvant tamoxifen prevalence in women with early breast cancer; monitoring recommended
• Breast cancer, Advanced, postmenopausal, following • Hepatic: Grade 3 or 4 elevations in liver enzymes have been reported
progression on tamoxifen therapy • Immunologic: Grade 3 or 4 lymphocytopenia has been reported
• Musculoskeletal: Bone mineral density reductions have been reported;
monitoring recommended
• Special populations: Not indicated to treat breast cancer in premenopausal
women
• Special populations: Females of reproductive potential should use effective
contraception during treatment and for 1 month after the last dose; may cause
fetal harm
Pregnancy Category
Fetal harm has been demonstrated. (MDX)
Breast Feeding
Micromedex: Infant risk cannot be ruled out.

Side Effects Contraindications

May include alopecia, diaphoresis, menopausal flushing , Hypersensitivity to exemestane or any component of the product
Increased appetite , nausea, arthralgia, headache, Insomnia,
depression, anxiety, fatigue.

Adult Dosing Pediatric dose

• Important Note • The safety and effectiveness in pediatric patients have not been established
◦ Routinely assess 25-hydroxy vitamin D levels prior to initiating
therapy and provide vitamin D supplementation to patients with
vitamin D deficiency.
• Breast cancer, Adjuvant, postmenopausal, estrogen receptor-
positive, following 2 to 3 years of adjuvant tamoxifen
◦ 25 mg orally once daily after a meal; initiate after 2 to 3 years
of tamoxifen and continue for completion of 5 consecutive years
of adjuvant endocrine therapy (FDA dosage)
◦ Duration of therapy, individualize and consider extended
duration of treatment with 10 years of adjuvant endocrine therapy
as follows: Aromatase inhibitor for 10 years; or tamoxifen for 2 to
3 years followed by aromatase inhibitor for 7 to 8 years; or
tamoxifen for 5 years followed by aromatase inhibitor for 5 years
(guideline dosage).
• Breast cancer, Adjuvant, premenopausal, in combination with
ovarian suppression
◦ 25 mg/day orally for 5 years plus ovarian suppression
(triptorelin 3.75 mg IM every 28 days, bilateral oophorectomy, or
ovarian irradiation) (off-label dosage)
• Breast cancer, Advanced, postmenopausal, following
progression on tamoxifen therapy
◦ 25 mg orally once daily after a meal
Drug classification Supplied
• Antineoplastic Agent • Generic
• Aromatase Inhibitor ◦ Oral Tablet: 25 MG
• Aromasin
◦ Oral Tablet: 25 MG

• Breast cancer, Invasive, in postmenopausal women at increased

risk; Prophylaxis
◦ 25 mg orally daily for 5 years (guideline dosage)
◦ 25 mg orally daily (off-label dosage)
• Breast cancer, Neoadjuvant, postmenopausal, hormone-receptor
positive
◦ 25 mg ORALLY once daily for 4 to 6 months prior to surgery
was used in clinical trials; international expert panel recommends
3 to 6 months of therapy

Pa
tir
o
mer (Veltassa®)
Drug classification Supplied
-Exchange resin Veltassa: Oral Powder for Suspension: 8.4 GM/1 Packet, 16.8 GM/1 Packet,
25.2 GM/1 Packet

Mechanism of Action Metabolism

Patiromer is a non-absorbed, cation exchange polymer containing Not available.
a calcium-sorbitol counterion. Potassium is bound in the
gastrointestinal tract lumen, which reduces potassium serum Elimination
levels through increased fecal excretion of potassium. Patiromer is excreted entirely in the feces.

Indications Percautions
FDA-Labeled indication  Endocrine/metabolic: Hypomagnesemia may occur; monitoring
Hyperkalemia recommended and magnesium supplementation may be required.

 Gastrointestinal: Gastrointestinal motility may become worse and result

in decreased efficacy; avoid use in patients with severe constipation,
bowel obstruction, or bowel impaction, including abnormal
postoperative bowel motility disorders.

Side Effects Contraindications

Common History of hypersensitivity reaction to patiromer or any product components.
-Gastrointestinal: Constipation (7.2%)
Serious
-Endocrine metabolic:Hypomagnesemia (5.3% to 9%)
-Gastrointestinal:Abnormal gastric motility

Adult Dosing Pediatric Dosing

Hyperkalemia Safety and efficacy not established in pediatric patients.
1- Initial, 8.4 g orally once daily.
2- Increase or decrease in increments of 8.4 g at 1-week or
longer intervals to achieve desired serum potassium level;
MAX, 25.2 g once daily

Dose Adjustments
Renal impairment: No adjustment required
BARICITINIB (Olumiant®)

Drug classification Supplied

-Janus kinase (JAK) inhibitor Olumiant 4mg, 2mg, 1mg tablets.

Mechanism of Action Metabolism

Baricitinib is Janus kinase inhibitor that reduces the phosphorylation and Inhibitor of OAT1, OAT2, OAT3, OCT 1, OCT2, OATP1B3, BCRP, and MATE 1 and
activation of signal transducers and activator of transcription responsible MATE2-K (no clinically relevant interactions)
for cytokines and growth factors involved in hematopoiesis, inflammation, Substrate of CYP3A4, P-gp, BCRP, MATE2-K, and OAT3; use with strong OAT3
and immune function. inhibitors not recommended
Elimination Half Life
•10 to 16 hours

Indications Percautions

FDA-Labeled Indications  Hepatic: Elevation of liver enzymes has been reported; monitoring required;
Alopecia areata (Severe) therapy interruption may be needed
COVID-19, In hospitalized patients requiring supplemental oxygen, non-  Cancer: Malignancies were observed in clinical studies of baricitinib. Increased
invasive or invasive mechanical ventilation, or extracorporeal membrane risk of malignancies, including lymphomas and lung cancers.
oxygenation (ECMO)  Cardiovascular: Increased risk of major adverse cardiovascular (CV) events
Rheumatoid arthritis (Moderate to Severe), Active, with inadequate (defined as cardiovascular death, non-fatal myocardial infarction (MI), and
response or intolerance to 1 or more TNF blockers. non-fatal stroke.
 Dermatologic: Non-melanoma skin cancers have been reported; monitoring
Non-FDA Labeled Indications recommended.
Atopic dermatitis (Moderate to Severe), In patients whom conventional  Hematologic: Thrombosis, including DVT and pulmonary embolism (PE), has
treatment is ineffective been observed

Side Effects Contraindications

Common • Specific contraindications have not been determined.
 Dermatologic: Acne, Folliculitis, Herpes zoster.
 Endocrine metabolic: Hyperlipidemia, Weight gain.
 Gastrointestinal: Abdominal pain, Nausea.
 Hepatic: Liver enzymes level above reference range.
 Musculoskeletal: Creatine kinase level above reference range.
 Neurologic: Headache.
 Reproductive: Candida infection of genital region.
 Respiratory:Lower and lower respiratory tract infection
Serious
 Cardiovascular:Myocardial infarction, Nonfatal, Sudden
cardiac death
 Gastrointestinal:Gastrointestinal perforation.
 Hematologic:Arterial thrombosis, Deep venous thrombosis,
Thrombosis, Venous thromboembolism.
 Immunologic:Hypersensitivity reaction.
 Neurologic:Cerebrovascular accident, Nonfatal.
 Respiratory:Pulmonary embolism.

Adult dose Pediatric dose

 Alopecia areata (Severe) • Safety and efficacy have not been established in pediatric patients.
2 mg orally once daily; increase to 4 mg orally once daily if response is not
adequate.
 Atopic dermatitis (Moderate to Severe), In patients whom
conventional treatment is ineffective
4 mg orally once daily used in combination with topical anti-inflammatory
agents (eg, topical steroids) and moisturizers.
 COVID-19, In hospitalized patients requiring supplemental
oxygen, non-invasive or invasive mechanical ventilation, or
extracorporeal membrane oxygenation (ECMO)
4 mg orally once daily for 14 days or until hospital discharge.
 Rheumatoid arthritis (Moderate to Severe), Active, with
inadequate response or intolerance to 1 or more TNF blockers
2 mg orally once daily as monotherapy or in combination with methotrexate
or other disease-modifying antirheumatic drugs (DMARDs)