Sunday, August 1, 2010

Amlodipine

MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
AmLODIPine may be confused with aMILoride
Norvasc® may be confused with Navane®, Norvir®, Vascor®

U.S. BRAND NAMES — Norvasc®

PHARMACOLOGIC CATEGORY
Calcium Channel Blocker
Calcium Channel Blocker, Dihydropyridine

DOSING: ADULTS
Hypertension: Oral: Initial dose: 5 mg once daily; maximum dose: 10 mg once daily. In general, titrate in 2.5 mg increments over 7-14 days. Usual dosage range (JNC 7): 2.5-10 mg once daily.

Angina: Oral: Usual dose: 5-10 mg; lower dose suggested in elderly or hepatic impairment; most patients require 10 mg for adequate effect.

DOSING: PEDIATRIC — Hypertension: Oral: Children 6-17 years: 2.5-5 mg once daily

(For additional information see "Amlodipine: Pediatric drug information")

DOSING: ELDERLY — Dosing should start at the lower end of dosing range due to possible increased incidence of hepatic, renal, or cardiac impairment. Elderly patients also show decreased clearance of amlodipine.

Hypertension: Oral: 2.5 mg once daily

Angina: Oral: 5 mg once daily

DOSING: RENAL IMPAIRMENT — Dialysis: Hemodialysis and peritoneal dialysis do not enhance elimination. Supplemental dose is not necessary.

DOSING: HEPATIC IMPAIRMENT
Hypertension: Administer 2.5 mg once daily

Angina: Administer 5 mg once daily

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet: 2.5 mg, 5 mg, 10 mg
Norvasc®: 2.5 mg, 5 mg, 10 mg

DOSAGE FORMS: CONCISE
Tablet: 2.5 mg, 5 mg, 10 mg
Norvasc®: 2.5 mg, 5 mg, 10 mg

GENERIC EQUIVALENT AVAILABLE — Yes

ADMINISTRATION — May be administered without regard to meals.

USE — Treatment of hypertension; treatment of symptomatic chronic stable angina, vasospastic (Prinzmetal's) angina (confirmed or suspected); prevention of hospitalization due to angina with documented CAD (limited to patients without heart failure or ejection fraction <40%)>10%: Cardiovascular: Peripheral edema (2% to 15% dose related)

1% to 10%:
Cardiovascular: Flushing (1% to 3%), palpitation (1% to 4%)
Central nervous system: Headache (7%; similar to placebo 8%), dizziness (1% to 3%), fatigue (4%), somnolence (1% to 2%)
Dermatologic: Rash (1% to 2%), pruritus (1% to 2%)
Endocrine & metabolic: Male sexual dysfunction (1% to 2%)
Gastrointestinal: Nausea (3%), abdominal pain (1% to 2%), dyspepsia (1% to 2%), gingival hyperplasia
Neuromuscular & skeletal: Muscle cramps (1% to 2%), weakness (1% to 2%)
Respiratory: Dyspnea (1% to 2%), pulmonary edema (15% from PRAISE trial, CHF population)

<1%>90%) to inactive metabolite

Bioavailability: 64% to 90%

Half-life elimination: 30-50 hours; increased with hepatic dysfunction

Time to peak, plasma: 6-12 hours

Excretion: Urine (10% as parent, 60% as metabolite)

PATIENT INFORMATION — Take as prescribed; do not stop abruptly without consulting prescriber. You may experience headache (if unrelieved, consult prescriber), nausea or vomiting (frequent small meals may help), or constipation (increased dietary bulk and fluids may help). May cause drowsiness; use caution when driving or engaging in tasks that require alertness until response to drug is known. Report unrelieved headache, vomiting, constipation, palpitations, peripheral or facial swelling, weight gain >5 lb/week, or respiratory changes.

Amlodipine

MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
AmLODIPine may be confused with aMILoride
Norvasc® may be confused with Navane®, Norvir®, Vascor®

U.S. BRAND NAMES — Norvasc®

PHARMACOLOGIC CATEGORY
Calcium Channel Blocker
Calcium Channel Blocker, Dihydropyridine

DOSING: ADULTS
Hypertension: Oral: Initial dose: 5 mg once daily; maximum dose: 10 mg once daily. In general, titrate in 2.5 mg increments over 7-14 days. Usual dosage range (JNC 7): 2.5-10 mg once daily.

Angina: Oral: Usual dose: 5-10 mg; lower dose suggested in elderly or hepatic impairment; most patients require 10 mg for adequate effect.

DOSING: PEDIATRIC — Hypertension: Oral: Children 6-17 years: 2.5-5 mg once daily

(For additional information see "Amlodipine: Pediatric drug information")

DOSING: ELDERLY — Dosing should start at the lower end of dosing range due to possible increased incidence of hepatic, renal, or cardiac impairment. Elderly patients also show decreased clearance of amlodipine.

Hypertension: Oral: 2.5 mg once daily

Angina: Oral: 5 mg once daily

DOSING: RENAL IMPAIRMENT — Dialysis: Hemodialysis and peritoneal dialysis do not enhance elimination. Supplemental dose is not necessary.

DOSING: HEPATIC IMPAIRMENT
Hypertension: Administer 2.5 mg once daily

Angina: Administer 5 mg once daily

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet: 2.5 mg, 5 mg, 10 mg
Norvasc®: 2.5 mg, 5 mg, 10 mg

DOSAGE FORMS: CONCISE
Tablet: 2.5 mg, 5 mg, 10 mg
Norvasc®: 2.5 mg, 5 mg, 10 mg

GENERIC EQUIVALENT AVAILABLE — Yes

ADMINISTRATION — May be administered without regard to meals.

USE — Treatment of hypertension; treatment of symptomatic chronic stable angina, vasospastic (Prinzmetal's) angina (confirmed or suspected); prevention of hospitalization due to angina with documented CAD (limited to patients without heart failure or ejection fraction <40%)>10%: Cardiovascular: Peripheral edema (2% to 15% dose related)

1% to 10%:
Cardiovascular: Flushing (1% to 3%), palpitation (1% to 4%)
Central nervous system: Headache (7%; similar to placebo 8%), dizziness (1% to 3%), fatigue (4%), somnolence (1% to 2%)
Dermatologic: Rash (1% to 2%), pruritus (1% to 2%)
Endocrine & metabolic: Male sexual dysfunction (1% to 2%)
Gastrointestinal: Nausea (3%), abdominal pain (1% to 2%), dyspepsia (1% to 2%), gingival hyperplasia
Neuromuscular & skeletal: Muscle cramps (1% to 2%), weakness (1% to 2%)
Respiratory: Dyspnea (1% to 2%), pulmonary edema (15% from PRAISE trial, CHF population)

<1%>90%) to inactive metabolite

Bioavailability: 64% to 90%

Half-life elimination: 30-50 hours; increased with hepatic dysfunction

Time to peak, plasma: 6-12 hours

Excretion: Urine (10% as parent, 60% as metabolite)

PATIENT INFORMATION — Take as prescribed; do not stop abruptly without consulting prescriber. You may experience headache (if unrelieved, consult prescriber), nausea or vomiting (frequent small meals may help), or constipation (increased dietary bulk and fluids may help). May cause drowsiness; use caution when driving or engaging in tasks that require alertness until response to drug is known. Report unrelieved headache, vomiting, constipation, palpitations, peripheral or facial swelling, weight gain >5 lb/week, or respiratory changes.

Amlexanox

U.S. BRAND NAMES — Aphthasol®

PHARMACOLOGIC CATEGORY
Anti-inflammatory, Locally Applied

DOSING: ADULTS — Aphthous ulcers: Topical: Administer ~1/4 inch (0.5 cm) directly on ulcers 4 times/day following oral hygiene, after meals, and at bedtime.

DOSING: ELDERLY — Refer to adult dosing.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Paste, oral:
Aphthasol®: 5% (3 g) [contains benzyl alcohol]

DOSAGE FORMS: CONCISE
Paste, oral:
Aphthasol®: 5% (3 g)

GENERIC EQUIVALENT AVAILABLE — No

USE — Treatment of aphthous ulcers (ie, canker sores)

USE - UNLABELED / INVESTIGATIONAL — Allergic disorders

ADVERSE REACTIONS SIGNIFICANT
1% to 2%:
Dermatologic: Allergic contact dermatitis
Gastrointestinal: Oral irritation

<1% (Limited to important or life-threatening): Contact mucositis

CONTRAINDICATIONS — Hypersensitivity to amlexanox or any component of the formulation

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Mucositis: Discontinue therapy if contact mucositis develops. Rash: Discontinue therapy if rash develops.

Special populations: Pediatrics: Safety and efficacy have not been established in children.

DRUG INTERACTIONS — There are no known significant interactions.

PREGNANCY RISK FACTOR — B (show table)

PREGNANCY IMPLICATIONS — Due to lack of data, avoid use in pregnancy, if possible.

LACTATION — Excretion in breast milk unknown/use caution

PRICING — (data from drugstore.com)
Paste (Aphthasol)
5% (3): $29.99

INTERNATIONAL BRAND NAMES — Elics (JP); Solfa (JP)

MECHANISM OF ACTION — As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox has anti-inflammatory and antiallergic properties; it inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3

PHARMACODYNAMICS / KINETICS
Absorption: Some from swallowed paste

Metabolism: Hydroxylated and conjugated metabolites

Half-life elimination: 3.5 hours

Time to peak, serum: 2 hours

Excretion: Urine (17% as unchanged drug)

Amlexanox

U.S. BRAND NAMES — Aphthasol®

PHARMACOLOGIC CATEGORY
Anti-inflammatory, Locally Applied

DOSING: ADULTS — Aphthous ulcers: Topical: Administer ~1/4 inch (0.5 cm) directly on ulcers 4 times/day following oral hygiene, after meals, and at bedtime.

DOSING: ELDERLY — Refer to adult dosing.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Paste, oral:
Aphthasol®: 5% (3 g) [contains benzyl alcohol]

DOSAGE FORMS: CONCISE
Paste, oral:
Aphthasol®: 5% (3 g)

GENERIC EQUIVALENT AVAILABLE — No

USE — Treatment of aphthous ulcers (ie, canker sores)

USE - UNLABELED / INVESTIGATIONAL — Allergic disorders

ADVERSE REACTIONS SIGNIFICANT
1% to 2%:
Dermatologic: Allergic contact dermatitis
Gastrointestinal: Oral irritation

<1% (Limited to important or life-threatening): Contact mucositis

CONTRAINDICATIONS — Hypersensitivity to amlexanox or any component of the formulation

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Mucositis: Discontinue therapy if contact mucositis develops. Rash: Discontinue therapy if rash develops.

Special populations: Pediatrics: Safety and efficacy have not been established in children.

DRUG INTERACTIONS — There are no known significant interactions.

PREGNANCY RISK FACTOR — B (show table)

PREGNANCY IMPLICATIONS — Due to lack of data, avoid use in pregnancy, if possible.

LACTATION — Excretion in breast milk unknown/use caution

PRICING — (data from drugstore.com)
Paste (Aphthasol)
5% (3): $29.99

INTERNATIONAL BRAND NAMES — Elics (JP); Solfa (JP)

MECHANISM OF ACTION — As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox has anti-inflammatory and antiallergic properties; it inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3

PHARMACODYNAMICS / KINETICS
Absorption: Some from swallowed paste

Metabolism: Hydroxylated and conjugated metabolites

Half-life elimination: 3.5 hours

Time to peak, serum: 2 hours

Excretion: Urine (17% as unchanged drug)

Wednesday, July 14, 2010

Amlexanox

U.S. BRAND NAMES — Aphthasol®

PHARMACOLOGIC CATEGORY
Anti-inflammatory, Locally Applied

DOSING: ADULTS — Aphthous ulcers: Topical: Administer ~1/4 inch (0.5 cm) directly on ulcers 4 times/day following oral hygiene, after meals, and at bedtime.

DOSING: ELDERLY — Refer to adult dosing.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Paste, oral:
Aphthasol®: 5% (3 g) [contains benzyl alcohol]

DOSAGE FORMS: CONCISE
Paste, oral:
Aphthasol®: 5% (3 g)

GENERIC EQUIVALENT AVAILABLE — No

USE — Treatment of aphthous ulcers (ie, canker sores)

USE - UNLABELED / INVESTIGATIONAL — Allergic disorders

ADVERSE REACTIONS SIGNIFICANT
1% to 2%:
Dermatologic: Allergic contact dermatitis
Gastrointestinal: Oral irritation

<1% (Limited to important or life-threatening): Contact mucositis

CONTRAINDICATIONS — Hypersensitivity to amlexanox or any component of the formulation

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Mucositis: Discontinue therapy if contact mucositis develops. Rash: Discontinue therapy if rash develops.

Special populations: Pediatrics: Safety and efficacy have not been established in children.

DRUG INTERACTIONS — There are no known significant interactions.

PREGNANCY RISK FACTOR — B (show table)

PREGNANCY IMPLICATIONS — Due to lack of data, avoid use in pregnancy, if possible.

LACTATION — Excretion in breast milk unknown/use caution

PRICING — (data from drugstore.com)
Paste (Aphthasol)
5% (3): $29.99

INTERNATIONAL BRAND NAMES — Elics (JP); Solfa (JP)

MECHANISM OF ACTION — As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox has anti-inflammatory and antiallergic properties; it inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3

PHARMACODYNAMICS / KINETICS
Absorption: Some from swallowed paste

Metabolism: Hydroxylated and conjugated metabolites

Half-life elimination: 3.5 hours

Time to peak, serum: 2 hours

Excretion: Urine (17% as unchanged drug)