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Brimonidine Tartrate
Overview
What is Brimonidine Tartrate?
Brimonidine Tartrate Ophthalmic Solution, 0.15% (1.5 mg
brimonidine tartrate per mL equivalent to 1.0 mg brimonidine free base per mL)
is a relatively selective alpha-2-adrenergic agonist for ophthalmic use. The
chemical name of brimonidine tartrate is 5-bromo-6-(2-imidazolidinylideneamino)
quinoxaline L-tartrate. It is an off-white to pale yellow powder. It has a
molecular weight of 442.24 as the tartrate salt, and is both soluble in water
(1.5 mg/mL) and in the product vehicle (3.0 mg/mL) at pH 7.2. The structural
formula is:
In solution, Brimonidine Tartrate Ophthalmic Solution, 0.15% has a clear,
greenish-yellow color. It has an osmolality of 250 - 350 mOsmol/kg and a pH of
6.6-7.4.
Each mL of Brimonidine Tartrate Ophthalmic Solution, 0.15% contains: brimonidine tartrate 0.15% (1.5 mg/mL)
povidone; boric acid; sodium borate; calcium
chloride; magnesium chloride; potassium chloride; mannitol; sodium chloride;
POLYQUAD* 0.001% (0.01 mg/mL); purified water; with hydrochloric acid and/or
sodium hydroxide to adjust pH.
What does Brimonidine Tartrate look like?
What are the available doses of Brimonidine Tartrate?
Sorry No records found.
What should I talk to my health care provider before I take Brimonidine Tartrate?
Sorry No records found
How should I use Brimonidine Tartrate?
Brimonidine Tartrate Ophthalmic Solution, 0.15% is indicated for the lowering of
intraocular pressure in patients with open-angle glaucoma or ocular
hypertension.
The recommended dose is one drop of Brimonidine Tartrate
Ophthalmic Solution, 0.15% in the affected eye(s) three-times-daily,
approximately 8 hours apart.
Brimonidine Tartrate Ophthalmic Solution, 0.15% may be used concomitantly
with other topical ophthalmic drug products to lower intraocular pressure. If
more than one topical ophthalmic product is being used, the products should be
administered at least 5 minutes apart.
What interacts with Brimonidine Tartrate?
Brimonidine Tartrate Ophthalmic Solution, 0.15% is contraindicated in patients with hypersensitivity to brimonidine tartrate or any component of this medication. It is also contraindicated in patients receiving monoamine oxidase (MAO) inhibitor therapy.
What are the warnings of Brimonidine Tartrate?
Sorry No Records found
What are the precautions of Brimonidine Tartrate?
Although Brimonidine Tartrate Ophthalmic Solution, 0.15% had
minimal effect on the blood pressure of patients in clinical studies, caution
should be exercised in treating patients with severe cardiovascular disease.
Brimonidine Tartrate Ophthalmic Solution, 0.15% has not been studied in
patients with hepatic or renal impairment; caution should be used in treating
such patients.
Brimonidine Tartrate Ophthalmic Solution, 0.15% should be used with caution
in patients with depression, cerebral or coronary insufficiency, Raynaud's
phenomenon, orthostatic hypotension, or thromboangiitis obliterans. Patients
prescribed IOP-lowering medication should be routinely monitored for IOP.
As with other drugs in this class, Brimonidine Tartrate
Ophthalmic Solution, 0.15% may cause fatigue and/or drowsiness in some patients.
Patients who engage in hazardous activities should be cautioned of the potential
for a decrease in mental alertness.
Although specific drug interaction studies have not been
conducted with Brimonidine Tartrate Ophthalmic Solution, 0.15%, the possibility
of an additive or potentiating effect with CNS depressants (alcohol,
barbiturates, opiates, sedatives, or anesthetics) should be considered. Alpha-2
agonists, as a class, may reduce pulse and blood pressure. Caution in using
concomitant drugs such as beta-blockers (ophthalmic and systemic),
anti-hypertensives and/or cardiac glycosides is advised.
Tricyclic antidepressants have been reported to blunt the hypotensive effect
of systemic clonidine. It is not known whether the concurrent use of these
agents with Brimonidine Tartrate Ophthalmic Solution, 0.15% in humans can
interfere with its IOP-lowering effect. No data on the level of circulating
catecholamines after Brimonidine Tartrate Ophthalmic Solution, 0.15%
administration are available. Caution, however, is advised in patients taking
tricyclic antidepressants, which can affect the metabolism and uptake of
circulating amines.
No compound-related carcinogenic effects were observed in either
mice or rats following a 21-month and a 24-month study, respectively. In these
studies, dietary administration of brimonidine tartrate at doses up to
2.5 mg/kg/day in mice and 1.0 mg/kg/day in rats achieved 60 and 50 times,
respectively, the plasma drug concentration estimated in humans treated with one
drop of Brimonidine Tartrate Ophthalmic Solution, 0.15% into both eyes.
Brimonidine tartrate was not mutagenic or cytogenic in a series of and studies
including the Ames test, chromosomal aberration assay in Chinese hamster ovary
(CHO) cells, a host-mediated assay and cytogenic studies in mice, and dominant
lethal assay.
Reproductive studies performed in rats and rabbits with oral
doses of 0.66 mg base/kg revealed no evidence of harm to the fetus due to
Brimonidine Tartrate Ophthalmic Solution, 0.15%. Dosing at this level produced
an exposure in rats and rabbits that is 80 and 40 times higher than the exposure
seen in humans, respectively.
There are no adequate and well-controlled studies in pregnant women. In
animal studies, brimonidine crossed the placenta and entered into the fetal
circulation to a limited extent. Brimonidine Tartrate Ophthalmic Solution, 0.15%
should be used during pregnancy only if the potential benefit to the mother
justifies the potential risk to the fetus.
It is not known whether this drug is excreted in human milk. In
animal studies, brimonidine tartrate was excreted in breast milk. A decision
should be made whether to discontinue nursing or to discontinue the drug, taking
into account the importance of the drug to the mother.
In a well-controlled clinical study conducted in pediatric
glaucoma patients (ages 2 to 7 years) the most commonly observed adverse events
with brimonidine tartrate ophthalmic solution 0.2% dosed three-times-daily were
somnolence (50%-83% in patients ages 2 to 6 years) and decreased alertness. In
pediatric patients 7 years of age or older (>20 kg), somnolence appears to
occur less frequently (25%). Approximately 16% of patients on brimonidine
tartrate ophthalmic solution discontinued from the study due to somnolence.
The safety and effectiveness of brimonidine tartrate ophthalmic solution have
not been studied in pediatric patients below the age of 2 years. Brimonidine
tartrate ophthalmic solution is not recommended for use in pediatric patients
under the age of 2 years. (Also refer to section.)
No overall differences in safety or effectiveness have been
observed between elderly and other adult patients.
What are the side effects of Brimonidine Tartrate?
Adverse events occurring in approximately 10-20% of the subjects
included: allergic conjunctivitis, conjunctival hyperemia, and eye pruritis.
Adverse events occurring in approximately 5-9% of the subjects included:
burning sensation, conjunctival folliculosis, hypertension, ocular allergic
reaction, oral dryness, and visual disturbance.
Events occurring in approximately 1-4% of subjects included: allergic
reaction, arthralgia, arthritis, asthenia, blepharitis, blepharoconjunctivitis,
blurred vision, bronchitis, cataract, chest pain, conjunctival edema,
conjunctival hemorrhage, conjunctivitis, cough, dizziness, diabetes mellitus,
dyspepsia, dyspnea, epiphora, eye discharge, eye dryness, eye irritation, eye
pain, eyelid edema, eyelid erythema, fatigue, flu syndrome, follicular
conjunctivitis, foreign body sensation, gastrointestinal disorder, headache,
hypercholesterolemia, hypotension, infection, insomnia, joint disorder,
keratitis, lid disorder, osteoporosis, pharyngitis, photophobia, rash, rhinitis,
sinus infection, sinusitis, somnolence, stinging, superficial punctate
keratopathy, tearing, visual field defect, vitreous detachment, vitreous
disorder, vitreous floaters, and worsened visual acuity.
The following events were reported in less than 1% of subjects: corneal
erosion, nasal dryness, and taste perversion.
The following events have been identified during post-marketing use of
brimonidine tartrate ophthalmic solutions in clinical practice. Because they are
reported voluntarily from a population of unknown size, estimates of frequency
cannot be made. The events, which have been chosen for inclusion due to either
their seriousness, frequency of reporting, possible causal connection to
brimonidine tartrate ophthalmic solutions, or a combination of these factors,
include: bradycardia; iritis; miosis; skin reactions (including erythema, eyelid
pruritis, rash, and vasodilation); and tachycardia. Apnea, bradycardia,
hypotension, hypothermia, hypotonia, and somnolence have been reported in
infants receiving brimonidine tartrate ophthalmic solutions.
What should I look out for while using Brimonidine Tartrate?
Brimonidine Tartrate Ophthalmic Solution, 0.15% is contraindicated in patients
with hypersensitivity to brimonidine tartrate or any component of this
medication. It is also contraindicated in patients receiving monoamine oxidase
(MAO) inhibitor therapy.
What might happen if I take too much Brimonidine Tartrate?
No information is available on overdosage in humans. Treatment of an oral
overdose includes supportive and symptomatic therapy; a patent airway should be
maintained.
How should I store and handle Brimonidine Tartrate?
Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP/NF with a child-resistant closure.A Schedule CIII Narcotic.Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP/NF with a child-resistant closure.A Schedule CIII Narcotic.Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP/NF with a child-resistant closure.A Schedule CIII Narcotic.Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008Brimonidine Tartrate Ophthalmic Solution, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows:10 mL in 10 mL bottle NDC 54868-6094-0Storage: Rx OnlyDistributed by:Falcon Pharmaceuticals, Ltd.Fort Worth, Texas 76134Manufactured by:Alcon Laboratories, Inc.Fort Worth, Texas 76134Printed in USA*POLYQUAD is a registered trademark of Alcon Research, Ltd.**ALPHAGAN P is a registered trademark of Allergan, Inc.349040-1008
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Brimonidine Tartrate Ophthalmic Solution, 0.15% is an alpha-2
adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring
at two hours post-dosing. Fluorophotometric studies in animals and humans
suggest that brimonidine tartrate has a dual mechanism of action by reducing
aqueous humor production and increasing uveoscleral outflow.
In a pharmacokinetic study, 14 healthy subjects (4 males and
10 females) received a single topical ocular administration of Brimonidine
Tartrate Ophthalmic Solution, 0.15%, one drop per eye. The peak plasma
concentrations (C) and AUC were 73 ± 19 pg/mL and 375 ± 89 pg•hr/mL, respectively. T was 1.7 ± 0.7 hours after dosing. The systemic half-life
was approximately 2.1 hours.
Brimonidine is metabolized primarily by the liver. metabolism data from human microsomal fractions and liver slices
indicate that brimonidine undergoes extensive hepatic metabolism.
Urinary excretion is the major route of elimination of brimonidine and its
metabolites. Approximately 87% of an orally administered radioactive dose of
brimonidine was eliminated within 120 hours, with 74% of the radioactivity
recovered in the urine.
Special Populations
Brimonidine Tartrate Ophthalmic Solution, 0.15% has not been studied in
patients with hepatic or renal impairment. Because of the low systemic drug
exposure following topical ocular administration of Brimonidine Tartrate
Ophthalmic Solution, 0.15%, no dose adjustment is necessary when treating
patients with hepatic or renal impairment.
Elevated IOP presents a major risk factor in glaucomatous field
loss. The higher the level of IOP, the greater the likelihood of optic nerve
damage and visual field loss. Brimonidine tartrate has the action of lowering
intraocular pressure with minimal effect on cardiovascular and pulmonary
parameters.
A clinical study was conducted to evaluate the safety and efficacy of
Brimonidine Tartrate Ophthalmic Solution, 0.15% compared to Alphagan® P**
administered three-times-daily in patients with open-angle glaucoma or ocular
hypertension. The results indicated that Brimonidine Tartrate Ophthalmic
Solution, 0.15% is equivalent in IOP-lowering effect to Alphagan® P (brimonidine
tartrate ophthalmic solution), 0.15%, and effectively lowers IOP in patients
with open-angle glaucoma or ocular hypertension by 2 - 6 mm Hg.
Non-Clinical Toxicology
Brimonidine Tartrate Ophthalmic Solution, 0.15% is contraindicated in patients with hypersensitivity to brimonidine tartrate or any component of this medication. It is also contraindicated in patients receiving monoamine oxidase (MAO) inhibitor therapy.CNS Drugs – Given the primary CNS effects of citalopram, caution should be used when it is taken in combination with other centrally acting drugs.
Alcohol – Although citalopram did not potentiate the cognitive and motor effects of alcohol in a clinical trial, as with other psychotropic medications, the use of alcohol by depressed patients taking citalopram is not recommended.
Monoamine Oxidase Inhibitors (MAOI’s) – See and .
Drugs That Interfere With Hemostasis (NSAIDs, Aspirin, Warfarin, etc.) – Serotonin release by platelets plays an important role in hemostasis. Epidemiological studies of the case-control and cohort design that have demonstrated an association between use of psychotropic drugs that interfere with serotonin reuptake and the occurrence of upper gastrointestinal bleeding have also shown that concurrent use of an NSAID or aspirin potentiated the risk of bleeding. Thus, patients should be cautioned about the use of such drugs concurrently with citalopram.
Cimetidine – In subjects who had received 21 days of 40 mg/day citalopram, combined administration of 400 mg/day cimetidine for 8 days resulted in an increase in citalopram AUC and C of 43% and 39%, respectively. The clinical significance of these findings is unknown.
Digoxin – In subjects who had received 21 days of 40 mg/day citalopram, combined administration of citalopram and digoxin (single dose of 1 mg) did not significantly affect the pharmacokinetics of either citalopram or digoxin.
Lithium – Coadministration of citalopram (40 mg/day for 10 days) and lithium (30 mmol/day for 5 days) had no significant effect on the pharmacokinetics of citalopram or lithium. Nevertheless, plasma lithium levels should be monitored with appropriate adjustment to the lithium dose in accordance with standard clinical practice. Because lithium may enhance the serotonergic effects of citalopram, caution should be exercised when citalopram and lithium are coadministered.
Pimozide – In a controlled study, a single dose of pimozide 2 mg coadministered with citalopram 40 mg given once daily for 11 days was associated with a mean increase in QTc values of approximately 10 msec compared to pimozide given alone. Citalopram did not alter the mean AUC or C of pimozide. The mechanism of this pharmacodynamic interaction is not known.
Theophylline – Combined administration of citalopram (40 mg/day for 21 days) and the CYP1A2 substrate theophylline (single dose of 300 mg) did not affect the pharmacokinetics of theophylline. The effect of theophylline on the pharmacokinetics of citalopram was not evaluated.
Sumatriptan – There have been rare postmarketing reports describing patients with weakness, hyperreflexia, and incoordination following the use of a selective serotonin reuptake inhibitor (SSRI) and sumatriptan. If concomitant treatment with sumatriptan and an SSRI (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram) is clinically warranted, appropriate observation of the patient is advised.
Warfarin – Administration of 40 mg/day citalopram for 21 days did not affect the pharmacokinetics of warfarin, a CYP3A4 substrate. Prothrombin time was increased by 5%, the clinical significance of which is unknown.
Carbamazepine – Combined administration of citalopram (40 mg/day for 14 days) and carbamazepine (titrated to 400 mg/day for 35 days) did not significantly affect the pharmacokinetics of carbamazepine, a CYP3A4 substrate. Although trough citalopram plasma levels were unaffected, given the enzyme inducing properties of carbamazepine, the possibility that carbamazepine might increase the clearance of citalopram should be considered if the two drugs are coadministered.
Triazolam – Combined administration of citalopram (titrated to 40 mg/day for 28 days) and the CYP3A4 substrate triazolam (single dose of 0.25 mg) did not significantly affect the pharmacokinetics of either citalopram or triazolam.
Ketoconazole – Combined administration of citalopram (40 mg) and ketoconazole (200 mg) decreased the C and AUC of ketoconazole by 21% and 10% respectively, and did not significantly affect the pharmacokinetics of citalopram.
CYP3A4 and 2C19 Inhibitors – studies indicated that CYP3A4 and 2C19 are the primary enzymes involved in the metabolism of citalopram. However, coadministration of citalopram (40 mg) and ketoconazole (200 mg), a potent inhibitor of CYP3A4, did not significantly affect the pharmacokinetics of citalopram. Because citalopram is metabolized by multiple enzyme systems, inhibition of a single enzyme may not appreciably decrease citalopram clearance.
Metoprolol – Administration of 40 mg/day citalopram for 22 days resulted in a two-fold increase in the plasma levels of the beta-adrenergic blocker metoprolol. Increased metoprolol plasma levels have been associated with decreased cardioselectivity. Coadministration of citalopram and metoprolol had no clinically significant effects on blood pressure or heart rate.
Imipramine and Other Tricyclic Antidepressants (TCAs) – studies suggest that citalopram is a relatively weak inhibitor of CYP2D6. Coadministration of citalopram (40 mg/day for 10 days) with the tricyclic antidepressant imipramine (single dose of 100 mg), a substrate for CYP2D6, did not significantly affect the plasma concentrations of imipramine or citalopram. However, the concentration of the imipramine metabolite desipramine was increased by approximately 50%. The clinical significance of the desipramine change is unknown. Nevertheless, caution is indicated in the coadministration of TCA’s with citalopram.
Electroconvulsive Therapy (ECT) – There are no clinical studies of the combined use of electroconvulsive therapy (ECT) and citalopram.
Although Brimonidine Tartrate Ophthalmic Solution, 0.15% had minimal effect on the blood pressure of patients in clinical studies, caution should be exercised in treating patients with severe cardiovascular disease.
Brimonidine Tartrate Ophthalmic Solution, 0.15% has not been studied in patients with hepatic or renal impairment; caution should be used in treating such patients.
Brimonidine Tartrate Ophthalmic Solution, 0.15% should be used with caution in patients with depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, or thromboangiitis obliterans. Patients prescribed IOP-lowering medication should be routinely monitored for IOP.
As with other drugs in this class, Brimonidine Tartrate Ophthalmic Solution, 0.15% may cause fatigue and/or drowsiness in some patients. Patients who engage in hazardous activities should be cautioned of the potential for a decrease in mental alertness.
Although specific drug interaction studies have not been conducted with Brimonidine Tartrate Ophthalmic Solution, 0.15%, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, or anesthetics) should be considered. Alpha-2 agonists, as a class, may reduce pulse and blood pressure. Caution in using concomitant drugs such as beta-blockers (ophthalmic and systemic), anti-hypertensives and/or cardiac glycosides is advised.
Tricyclic antidepressants have been reported to blunt the hypotensive effect of systemic clonidine. It is not known whether the concurrent use of these agents with Brimonidine Tartrate Ophthalmic Solution, 0.15% in humans can interfere with its IOP-lowering effect. No data on the level of circulating catecholamines after Brimonidine Tartrate Ophthalmic Solution, 0.15% administration are available. Caution, however, is advised in patients taking tricyclic antidepressants, which can affect the metabolism and uptake of circulating amines.
No compound-related carcinogenic effects were observed in either mice or rats following a 21-month and a 24-month study, respectively. In these studies, dietary administration of brimonidine tartrate at doses up to 2.5 mg/kg/day in mice and 1.0 mg/kg/day in rats achieved 60 and 50 times, respectively, the plasma drug concentration estimated in humans treated with one drop of Brimonidine Tartrate Ophthalmic Solution, 0.15% into both eyes.
Brimonidine tartrate was not mutagenic or cytogenic in a series of and studies including the Ames test, chromosomal aberration assay in Chinese hamster ovary (CHO) cells, a host-mediated assay and cytogenic studies in mice, and dominant lethal assay.
Reproductive studies performed in rats and rabbits with oral doses of 0.66 mg base/kg revealed no evidence of harm to the fetus due to Brimonidine Tartrate Ophthalmic Solution, 0.15%. Dosing at this level produced an exposure in rats and rabbits that is 80 and 40 times higher than the exposure seen in humans, respectively.
There are no adequate and well-controlled studies in pregnant women. In animal studies, brimonidine crossed the placenta and entered into the fetal circulation to a limited extent. Brimonidine Tartrate Ophthalmic Solution, 0.15% should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.
It is not known whether this drug is excreted in human milk. In animal studies, brimonidine tartrate was excreted in breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
In a well-controlled clinical study conducted in pediatric glaucoma patients (ages 2 to 7 years) the most commonly observed adverse events with brimonidine tartrate ophthalmic solution 0.2% dosed three-times-daily were somnolence (50%-83% in patients ages 2 to 6 years) and decreased alertness. In pediatric patients 7 years of age or older (>20 kg), somnolence appears to occur less frequently (25%). Approximately 16% of patients on brimonidine tartrate ophthalmic solution discontinued from the study due to somnolence.
The safety and effectiveness of brimonidine tartrate ophthalmic solution have not been studied in pediatric patients below the age of 2 years. Brimonidine tartrate ophthalmic solution is not recommended for use in pediatric patients under the age of 2 years. (Also refer to section.)
No overall differences in safety or effectiveness have been observed between elderly and other adult patients.
Adverse events occurring in approximately 10-20% of the subjects included: allergic conjunctivitis, conjunctival hyperemia, and eye pruritis.
Adverse events occurring in approximately 5-9% of the subjects included: burning sensation, conjunctival folliculosis, hypertension, ocular allergic reaction, oral dryness, and visual disturbance.
Events occurring in approximately 1-4% of subjects included: allergic reaction, arthralgia, arthritis, asthenia, blepharitis, blepharoconjunctivitis, blurred vision, bronchitis, cataract, chest pain, conjunctival edema, conjunctival hemorrhage, conjunctivitis, cough, dizziness, diabetes mellitus, dyspepsia, dyspnea, epiphora, eye discharge, eye dryness, eye irritation, eye pain, eyelid edema, eyelid erythema, fatigue, flu syndrome, follicular conjunctivitis, foreign body sensation, gastrointestinal disorder, headache, hypercholesterolemia, hypotension, infection, insomnia, joint disorder, keratitis, lid disorder, osteoporosis, pharyngitis, photophobia, rash, rhinitis, sinus infection, sinusitis, somnolence, stinging, superficial punctate keratopathy, tearing, visual field defect, vitreous detachment, vitreous disorder, vitreous floaters, and worsened visual acuity.
The following events were reported in less than 1% of subjects: corneal erosion, nasal dryness, and taste perversion.
The following events have been identified during post-marketing use of brimonidine tartrate ophthalmic solutions in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. The events, which have been chosen for inclusion due to either their seriousness, frequency of reporting, possible causal connection to brimonidine tartrate ophthalmic solutions, or a combination of these factors, include: bradycardia; iritis; miosis; skin reactions (including erythema, eyelid pruritis, rash, and vasodilation); and tachycardia. Apnea, bradycardia, hypotension, hypothermia, hypotonia, and somnolence have been reported in infants receiving brimonidine tartrate ophthalmic solutions.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72Tips
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Interactions
Interactions
A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).