Clinical Pharmacology

LAMOTRIGINE tablet [REMEDYREPACK INC.] | National Institutes of Health | 11/9/2020

… concentrations in controlled clinical trials in patients with epilepsy. Effect of Lamotrigine on Organic Cationic Transporter 2 Substrates Lamotrigine is an inhibitor of renal tubular secretion via organic cationic transporter 2 (OCT2) proteins [see Clinical Pharmacology ( 12.3 )] . This may result in increased plasma levels of certain drugs that are substantially excreted via this route. Coadministration of lamotrigine with OCT2 substrates with a narrow therapeutic index (e.g., dofetilide) is not recommended …

SERTRALINE HYDROCHLORIDE tablet, film coated [PD-Rx Pharmaceuticals, Inc.] | National Institutes of Health | 11/9/2020

… with sertraline hydrochloride overdose (single or multiple drugs) include bradycardia, bundle branch block, coma, convulsions, delirium, hallucinations, hypertension, hypotension, manic reaction, pancreatitis, QTc-interval prolongation, Torsade de Pointes, serotonin syndrome, stupor, and syncope [See Clinical Pharmacology (12.2) ]. Overdose Management 11 DESCRIPTION Sertraline hydrochloride tablets USP contains sertraline hydrochloride, an SSRI. Sertraline hydrochloride has a molecular weight of 342.7 and has the following chemical name: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4 …

BUPRENORPHINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE DIHYDRATE tablet [Bryant Ranch Prepack] | National Institutes of Health | 11/9/2020

… greater than one month of use. Anaphylaxis : Anaphylaxis has been reported with ingredients contained in buprenorphine and naloxone sublingual tablets. Androgen deficiency : Cases of androgen deficiency have occurred with chronic use of opioids [see Clinical Pharmacology (12.2) ] . Local reactions : Glossodynia, glossitis, oral mucosal erythema, oral hypoesthesia, and stomatitis. Table 3 includes clinically significant drug interactions with buprenorphine and naloxone sublingual tablets. Table 3. Clinically Significant Drug Interactions Benzodiazepines or Other …

NEOMYCIN POLYMYXIN B SULFATES AND DEXAMETHASONE (neomycin sulfate, polymyxin b sulfate and dexamethasone) suspension/ drops [Bausch & Lomb Incorporated] | National Institutes of Health | 11/9/2020

… to neomycin 3.5 mg, polymyxin B sulfate 10,000 units, dexamethasone 0.1%. Inactives: hypromellose 2910 0.5%, sodium chloride, polysorbate 20, hydrochloric acid and/or sodium hydroxide (to adjust pH), purified water, benzalkonium chloride 0.004% (preservative). CLINICAL PHARMACOLOGY Corticosteroids suppress the inflammatory response to a variety of agents and they probably delay or slow healing. Since corticosteroids may inhibit the body‚Äôs defense mechanism against infection, a concomitant antimicrobial drug may be …

KETOPROFEN capsule, extended release [Mylan Pharmaceuticals Inc.] | National Institutes of Health | 11/9/2020

… as a potential reservoir for parent drug, and this may be important in persons with renal insufficiency, whereby the conjugate may accumulate in the serum and undergo deconjugation back to the parent drug (see CLINICAL PHARMACOLOGY: Special Populations: Renally Impaired ). The conjugates are reported to appear only in trace amounts in plasma in healthy adults, but are higher in elderly subjects ‚Äî presumably because of reduced renal clearance. It has …

TESTOSTERONE CYPIONATE injection, solution [Sun Pharmaceutical Industries, Inc.] | National Institutes of Health | 11/6/2020

CLINICAL PHARMACOLOGY Endogenous androgens are responsible for normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include growth and maturation of the prostate, seminal vesicles, penis, and scrotum; development of male hair distribution, such as beard, pubic, chest, and axillary hair; laryngeal enlargement, vocal cord thickening, and alterations in body musculature and fat distribution. Drugs in this class also cause retention …

Sage Therapeutics Announces Third Quarter 2020 Financial Results and Highlights Pipeline and Business Progress | Business & Finance | manchestertimes.com | Business Wire | 11/5/2020

… initiated with a new open-label antidepressant, in patients with MDD, with additional short-term follow-up. Topline data from this study are anticipated in 2021. Sage is also currently evaluating the ongoing zuranolone clinical pharmacology and safety program and plans to finalize requirements to support a potential future new drug application (NDA) with the FDA. ZULRESSO ¬Æ (brexanolone) CIV injection: Revenue in the third quarter of 2020 from sales …

Sage Therapeutics Announces Third Quarter 2020 Financial Results and Highlights Pipeline and Business Progress - GuruFocus.com | 11/5/2020

… initiated with a new open-label antidepressant, in patients with MDD, with additional short-term follow-up. Topline data from this study are anticipated in 2021. Sage is also currently evaluating the ongoing zuranolone clinical pharmacology and safety program and plans to finalize requirements to support a potential future new drug application (NDA) with the FDA. ZULRESSO ¬Æ (brexanolone) CIV injection: Revenue in the third quarter of 2020 from sales …

METOPROLOL TARTRATE tablet, film coated [Advagen Pharma Limited] | National Institutes of Health | 11/4/2020

… mg of metoprolol tartrate and the following inactive ingredients: lactose monohydrate, colloidal silicon dioxide, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, titanium dioxide, sodium starch glycolate, talc and D & C Red 30 Aluminium Lake. CLINICAL PHARMACOLOGY Mechanism of Action Metoprolol is a beta 1 -selective (cardioselective) adrenergic receptor blocker. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta 2 adrenoreceptors, chiefly located in …

NOURIANZ (istradefylline) tablet, film coated [Kyowa Kirin, Inc.] | National Institutes of Health | 11/4/2020

… causal relationship to drug exposure: increased libido. 7.1 Effect of Other Drugs on NOURIANZ Strong CYP3A4 Inhibitors Coadministration of NOURIANZ with a strong CYP3A4 inhibitor (ketoconazole) increased istradefylline AUC inf by 2.5-fold [see Clinical Pharmacology (12.3) ] . Therefore, the recommended maximum dosage of NOURIANZ in patients concomitantly using strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, clarithromycin) is 20 mg once daily [see Dosage and Administration (2.2) ]. Strong CYP3A4 Inducers Coadministration of …

RAMELTEON tablet [DIRECT RX] | National Institutes of Health | 11/4/2020

… increased approximately 190-fold, and the Cmax increased approximately 70-fold upon coadministration of fluvoxamine and ramelteon, compared to ramelteon administered alone. Ramelteon should not be used in combination with fluvoxamine [see Contraindications (4), Clinical Pharmacology (12.5)]. Other less strong CYP1A2 inhibitors have not been adequately studied. Ramelteon should be administered with caution to patients taking less strong CYP1A2 inhibitors. Rifampin (strong CYP enzyme inducer) Administration of multiple doses of …

CYCLOBENZAPRINE HYDROCHLORIDE tablet, film coated [RedPharm Drug, Inc.] | National Institutes of Health | 11/4/2020

… stearate, microcrystalline cellulose, polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide. In addition, the 5 mg tablet contain FD&C yellow 6, and both the 5 mg and 10 mg tablets contain iron oxide yellow. CLINICAL PHARMACOLOGY Cyclobenzaprine hydrochloride relieves skeletal muscle spasm of local origin without interfering with muscle function. It is ineffective in muscle spasm due to central nervous system disease. Cyclobenzaprine reduced or abolished skeletal muscle hyperactivity in …

FLUCONAZOLE IN SODIUM CHLORIDE injection, solution [Hospira, Inc.] | National Institutes of Health | 11/4/2020

… study. Coadministration of other drugs known to prolong the QT interval and which are metabolized via the enzyme CYP3A4 such as cisapride, astemizole, erythromycin, pimozide, and quinidine are contraindicated in patients receiving fluconazole. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies and PRECAUTIONS ) WARNINGS 1. Hepatic Injury: Fluconazole should be administered with caution to patients with liver dysfunction. Fluconazole has been associated with rare cases of serious hepatic toxicity, including fatalities primarily …

Cognition Thinks It Has an Alzheimer’s Blockbuster | 11/3/2020

… clinic or heading that way? Catalano: Our lead drug candidate is CT1812, currently in four phase II clinical trials with a fifth about to start. These are studies where we are looking at the clinical pharmacology to understand the drug√¢‚Ǩ‚Ñ¢s mechanism of action and its impact on disease. These trials are all being done in patients with mild-to-moderate Alzheimer‚Äôs disease, with the exception of …

GALANTAMINE capsule, extended release [Actavis Pharma, Inc.] | National Institutes of Health | 11/3/2020

Galantamine has the potential to interfere with the activity of anticholinergic medications [see Clinical Pharmacology ( 12.3 )] . 7.2 Use with Cholinomimetics and Other Cholinesterase Inhibitors A synergistic effect is expected when cholinesterase inhibitors are given concurrently with succinylcholine, other cholinesterase inhibitors, similar neuromuscular blocking agents or cholinergic agonists such as bethanechol [see Clinical Pharmacology ( 12.3 )] . 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the …

HYDROCODONE BITARTRATE AND ACETAMINOPHEN tablet [RedPharm Drug, Inc.] | National Institutes of Health | 11/3/2020

325 mg 325 mg In addition each tablet contains the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, crospovidone, magnesium stearate, microcrystalline cellulose, povidone, pregelatinized starch and stearic acid. Meets USP Dissolution Test 1. CLINICAL PHARMACOLOGY Mechanism of Action Hydrocodone is full opioid agonist with relative selectivity for the mu-opioid (Œº) receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action of hydrocodone …

LORAZEPAM tablet [REMEDYREPACK INC.] | National Institutes of Health | 11/3/2020

… almost insoluble in water. Each lorazepam tablet, to be taken orally, contains 0.5 mg, 1 mg, or 2 mg of lorazepam. The inactive ingredients present are lactose, magnesium stearate, microcrystalline cellulose, and polacrilin potassium. CLINICAL PHARMACOLOGY Studies in healthy volunteers show that in single high doses lorazepam has a tranquilizing action on the central nervous system with no appreciable effect on the respiratory or cardiovascular systems. Lorazepam is readily absorbed …

ONDANSETRON tablet, orally disintegrating [Asclemed USA, Inc.] | National Institutes of Health | 11/2/2020

… treatment [see Warnings and Precautions (5.3) ] . 7.2 Drugs Affecting Cytochrome P-450 Enzymes Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver [see Clinical Pharmacology (12.3) ] . Because ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes (CYP3A4, CYP2D6, CYP1A2), inducers or inhibitors of these enzymes may change the clearance and, hence, the half-life of ondansetron. In …

DOXERCALCIFEROL capsule [Heritage Pharmaceuticals Inc. d/b/a Avet Pharmaceuticals Inc.] | National Institutes of Health | 11/2/2020

… Cytochrome P450 Inhibitors Clinical Impact Doxercalciferol is activated by CYP 27 in the liver. Cytochrome P450 inhibitors may inhibit the 25-hydroxylation of doxercalciferol and thus reduce the formation of active doxercalciferol moiety [see Clinical Pharmacology ( 12.3 )]. Examples Ketoconazole and erythromycin Intervention If a patient initiates or discontinues therapy with a cytochrome P450 inhibitor, dose adjustment of doxercalciferol may be necessary. Monitor intact PTH and serum calcium concentrations closely. Enzyme …

HYDROXYCHLOROQUINE SULFATE tablet [Dr. Reddy’s Laboratories Inc.] | National Institutes of Health | 11/2/2020

WARNINGS: Resistant strains of malaria: Hydroxychloroquine Sulfate Tablets are not effective against chloroquine-resistant strains of P. falciparum (see CLINICAL PHARMACOLOGY ‚Äì Microbiology ). Ocular: Irreversible retinal damage has been observed in some patients who had received hydroxychloroquine sulfate. Significant risk factors for retinal damage include daily doses of hydroxychloroquine sulfate greater than 6.5 mg/kg (5 mg/kg base) of actual body weight, durations of use greater than five years …

LOVASTATIN tablet [Denton Pharma, Inc. dba Northwind Pharmaceuticals] | National Institutes of Health | 11/2/2020

… WARNINGS , Myopathy/Rhabdomyolysis ). Danazol, Diltiazem, Dronedarone, or Verapamil: The risk of myopathy/rhabdomyolysis is increased by concomitant administration of danazol, diltiazem, dronedarone or verapamil particularly with higher doses of lovastatin (see WARNINGS , Myopathy/Rhabdomyolysis ; CLINICAL PHARMACOLOGY , Pharmacokinetics ). Amiodarone: The risk of myopathy/rhabdomyolysis is increased when amiodarone is used concomitantly with a closely related member of the HMG-CoA reductase inhibitor class (see WARNINGS , Myopathy/Rhabdomyolysis ). Coumarin Anticoagulants: In a …

TIZANIDINE tablet [Denton Pharma, Inc. dba Northwind Pharmaceuticals] | National Institutes of Health | 11/2/2020

… Fluvoxamine Concomitant use of fluvoxamine and tizanidine is contraindicated. Changes in pharmacokinetics of tizanidine when administered with fluvoxamine resulted in significantly decreased blood pressure, increased drowsiness, and increased psychomotor impairment. [see Contraindications ( 4 ) and Clinical Pharmacology ( 12.3 )] 7.2 Ciprofloxacin Concomitant use of ciprofoxacin and tizanidine is contraindicated. Changes in pharmacokinetics of tizanidine when administered with ciprofloxacin resulted in significantly decreased blood pressure, increased drowsiness, and increased psychomotor impairment [see Contraindications …

HYDROXYZINE HYDROCHLORIDE tablet, film coated [Denton Pharma, Inc. dba Northwind Pharmaceuticals] | National Institutes of Health | 11/2/2020

… C Red 40 Aluminum Lake (50 mg), FD&C Yellow 6 Aluminum Lake (10 mg and 50 mg), hypromellose, polyethylene glycol 3350, polyvinyl alcohol, talc, titanium dioxide, triacetin and yellow iron oxide (10 mg). CLINICAL PHARMACOLOGY Hydroxyzine hydrochloride is unrelated chemically to the phenothiazines, reserpine, meprobamate or the benzodiazepines. Hydroxyzine is not a cortical depressant, but its action may be due to a suppression of activity in certain key regions …

HYOSCYAMINE SULFATE tablet [Denton Pharma, Inc. dba Northwind Pharmaceuticals] | National Institutes of Health | 11/2/2020

… methyl-8-azabicyclo [3.2.1] oct-3-yl ester, [3(S)-endo]-, sulfate (2:1), dihydrate with the following structure: Each tablet also contains as inactive ingredients: Colloidal silicon dioxide, crospovidone, magnesium stearate and microcrystalline cellulose. CLINICAL PHARMACOLOGY Hyoscyamine sulfate inhibits specifically the actions of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in …

FAMOTIDINE tablet, film coated [RedPharm Drug, Inc.] | National Institutes of Health | 11/2/2020

… with famotidine. Since famotidine blood levels are higher in patients with renal impairment than in patients with normal renal function, dosage adjustments are recommended in patients with renal impairment [see Dosage and Administration (2.2) , Clinical Pharmacology (12.3) ]. 5.2 Concurrent Gastric Malignancy In adults, symptomatic response to therapy with famotidine does not preclude the presence of gastric malignancy. Consider evaluation for gastric malignancy in adult patients who have a suboptimal response …