Singapore Drugs Database

ABIRONE ABIRATERONE ACETATE TABLETS 250 MG

Admin — Sun, 20 Jun 2021 16:25:42 +0000

Product Information

Registration Status: Active

ABIRONE ABIRATERONE ACETATE TABLETS 250 MG is approved to be sold in Singapore with effective from 2021-06-16. It is marketed by Hetero Singapore Pte Ltd, with the registration number of SIN16239P.

This product contains Abiraterone 250.000 mg in the form of TABLET. It is approved for ORAL use.

This product is manufactured by Hetero Labs Limited in INDIA.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Abiraterone is a derivative of steroidal progesterone and is an innovative drug that offers clinical benefit to patients with hormone refractory prostate cancer. Abiraterone is administered as an acetate salt prodrug because it has a higher bioavailability and less susceptible to hydrolysis than abiraterone itself. FDA approved on April 28, 2011.

Indication

Used in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.

Mechanism of Action

Abiraterone is an orally active inhibitor of the steroidal enzyme CYP17A1 (17 alpha-hydroxylase/C17,20 lyase). It inhibits CYP17A1 in a selective and irreversible manner via covalent binding mechanism. CYP17A1 is an enzyme that catalyzes the biosynthesis of androgen and is highly expressed in testicular, adrenal, and prostatic tumor tissue. More specifically, abiraterone inhibits the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone (DHEA) by the enzyme CYP17A1 to decrease serum levels of testosterone and other androgens.

Pharmacokinetics

Absorption: Abiraterone itself is poorly absorbed and is susceptible to hydrolysis by esterases. The salt form, abiraterone acetate, is a prodrug which has a much higher oral bioavailability and is also esterase resistant. Peak drug concentrations of abiraterone were reached in 1.5 - 4 hours. Abiraterone acetate was rapidly and completely deacetylated into abiraterone-the parent salt form was not detectable in early pharmacokinetic studies. Food and high fat meals increases absorption 4.4-fold.
Distribution: Vdss= 19,669 ± 13,358 L
Metabolism: Abiraterone acetate is hydrolyzed into active metabolite abiraterone via esterases. CYP3A4 and SULT2A1 further metabolizes abiraterone into two inactive metabolites called abiraterone sulfate and N-oxide abiraterone sulfate.
Elimination

Toxicity

Toxicity is related to the blockade of 17α-hydroxylase activity. Blockade results in the accumulation of upstream mineralocorticoids like 11-deoxycorticosterone leading to secondary hyperaldosteronism. Signs of hydroaldosteronism include fluid retention and hypokalemia. Mineralocorticoid receptor antagonists may be used to treat signs and symptoms.

Active Ingredient/Synonyms

(3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-ol | 17-(3-Pyridyl)androsta-5,16-dien-3beta-ol | Abiraterone |

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post ABIRONE ABIRATERONE ACETATE TABLETS 250 MG appeared first on Singapore Drugs Database.

BENZATROPINE PHEBRA SOLUTION FOR INJECTION 2 MG/2 ML

Admin — Sun, 20 Jun 2021 16:25:40 +0000

Product Information

Registration Status: Active

BENZATROPINE PHEBRA SOLUTION FOR INJECTION 2 MG/2 ML is approved to be sold in Singapore with effective from 2021-06-03. It is marketed by PHEBRA (SE ASIA) PTE LTD, with the registration number of SIN16222P.

This product contains Benzatropine 2.0 mg/2ml in the form of INJECTION, SOLUTION. It is approved for INTRAVENOUS, INTRAMUSCULAR use.

This product is manufactured by Phebra Pty Ltd in AUSTRALIA.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson’s disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics (e.g. phenothiazines). Symptoms of Parkinson’s disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor.

Indication

For use as an adjunct in the therapy of all forms of parkinsonism and also for use in the control of extrapyramidal disorders due to neuroleptic drugs.

Mechanism of Action

Benztropine is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Benztropine partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement.

Pharmacokinetics

Absorption: Onset of action is 1-2 hours following oral administration. The onset of action is within minutes when administered by IM or IV injection.
Distribution
Metabolism
Elimination

Toxicity

Signs of overdose include confusion, nervousness, listlessness, hallucinations, dizziness; muscle weakness, ataxia, dry mouth, mydriasis, blurred vision, palpitations, tachycardia, elevated blood pressure, nausea, vomiting, dysuria, numbness of fingers, headache, delirium, coma, shock, convulsions, respiratory arrest, anhidrosis, hyperthermia, glaucoma, and constipation.

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post BENZATROPINE PHEBRA SOLUTION FOR INJECTION 2 MG/2 ML appeared first on Singapore Drugs Database.

COXETA FC TABLETS 60MG

Admin — Sun, 20 Jun 2021 16:25:39 +0000

Product Information

Registration Status: Active

COXETA FC TABLETS 60MG is approved to be sold in Singapore with effective from 2021-05-28. It is marketed by TEVA PHARMACEUTICAL INVESTMENTS SINGAPORE PTE LTD, with the registration number of SIN16213P.

This product contains Etoricoxib 60 mg in the form of TABLET, FILM COATED. It is approved for ORAL use.

This product is manufactured by TEVA Gyógyszergyár Zrt. (Teva Pharmaceutical Works Private Limited Company) in HUNGARY.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Etoricoxib is a new COX-2 selective inhibitor. Current therapeutic indications are: treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Like any other COX-2 selective inhibitor, Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces the generation of prostaglandins (PGs) from arachidonic acid.

Indication

For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

Mechanism of Action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.

Pharmacokinetics

Absorption: Bioavailability is 100% following oral administration.
Distribution
Metabolism: Hepatic, primarily via CYP3A4.
Elimination

Toxicity

This reduced activity is the cause of reduced gastrointestinal toxicity, as demonstrated in several large clinical trials performed with different COXIB (see below links on NEJM and The Lancet). Some clinical trials and meta-analysis showed that treatment with COXIB lead to increased incidence of cardiovascular adverse events compared to placebo

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post COXETA FC TABLETS 60MG appeared first on Singapore Drugs Database.

COXETA FC TABLETS 90MG

Admin — Sun, 20 Jun 2021 16:25:37 +0000

Product Information

Registration Status: Active

COXETA FC TABLETS 90MG is approved to be sold in Singapore with effective from 2021-05-28. It is marketed by TEVA PHARMACEUTICAL INVESTMENTS SINGAPORE PTE LTD, with the registration number of SIN16212P.

This product contains Etoricoxib 90 mg in the form of TABLET, FILM COATED. It is approved for ORAL use.

This product is manufactured by TEVA Gyógyszergyár Zrt. (Teva Pharmaceutical Works Private Limited Company) in HUNGARY.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Indication

For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

Mechanism of Action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.

Pharmacokinetics

Absorption: Bioavailability is 100% following oral administration.
Distribution
Metabolism: Hepatic, primarily via CYP3A4.
Elimination

Toxicity

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post COXETA FC TABLETS 90MG appeared first on Singapore Drugs Database.

ABIRONE ABIRATERONE ACETATE TABLETS 250 MG

Admin — Sun, 20 Jun 2021 16:25:36 +0000

Product Information

Registration Status: Active

Description

Indication

Used in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.

Mechanism of Action

Pharmacokinetics

Absorption: Abiraterone itself is poorly absorbed and is susceptible to hydrolysis by esterases. The salt form, abiraterone acetate, is a prodrug which has a much higher oral bioavailability and is also esterase resistant. Peak drug concentrations of abiraterone were reached in 1.5 - 4 hours. Abiraterone acetate was rapidly and completely deacetylated into abiraterone-the parent salt form was not detectable in early pharmacokinetic studies. Food and high fat meals increases absorption 4.4-fold.
Distribution: Vdss= 19,669 ± 13,358 L
Metabolism: Abiraterone acetate is hydrolyzed into active metabolite abiraterone via esterases. CYP3A4 and SULT2A1 further metabolizes abiraterone into two inactive metabolites called abiraterone sulfate and N-oxide abiraterone sulfate.
Elimination

Toxicity

Active Ingredient/Synonyms

(3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-ol | 17-(3-Pyridyl)androsta-5,16-dien-3beta-ol | Abiraterone |

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post ABIRONE ABIRATERONE ACETATE TABLETS 250 MG appeared first on Singapore Drugs Database.

COXETA FC TABLETS 120MG

Admin — Sun, 20 Jun 2021 16:25:36 +0000

Product Information

Registration Status: Active

COXETA FC TABLETS 120MG is approved to be sold in Singapore with effective from 2021-05-28. It is marketed by TEVA PHARMACEUTICAL INVESTMENTS SINGAPORE PTE LTD, with the registration number of SIN16211P.

This product contains Etoricoxib 120 mg in the form of TABLET, FILM COATED. It is approved for ORAL use.

This product is manufactured by TEVA Gyógyszergyár Zrt. (Teva Pharmaceutical Works Private Limited Company) in HUNGARY.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Indication

For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

Mechanism of Action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.

Pharmacokinetics

Absorption: Bioavailability is 100% following oral administration.
Distribution
Metabolism: Hepatic, primarily via CYP3A4.
Elimination

Toxicity

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post COXETA FC TABLETS 120MG appeared first on Singapore Drugs Database.

BENZATROPINE PHEBRA SOLUTION FOR INJECTION 2 MG/2 ML

Admin — Sun, 20 Jun 2021 16:25:35 +0000

Product Information

Registration Status: Active

Description

Indication

For use as an adjunct in the therapy of all forms of parkinsonism and also for use in the control of extrapyramidal disorders due to neuroleptic drugs.

Mechanism of Action

Pharmacokinetics

Absorption: Onset of action is 1-2 hours following oral administration. The onset of action is within minutes when administered by IM or IV injection.
Distribution
Metabolism
Elimination

Toxicity

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post BENZATROPINE PHEBRA SOLUTION FOR INJECTION 2 MG/2 ML appeared first on Singapore Drugs Database.

APROVASC FILM COATED TABLET 300MG/10MG

Admin — Sun, 20 Jun 2021 16:25:33 +0000

Product Information

Registration Status: Active

APROVASC FILM COATED TABLET 300MG/10MG is approved to be sold in Singapore with effective from 2021-05-14. It is marketed by SANOFI-AVENTIS SINGAPORE PTE LTD, with the registration number of SIN16196P.

This product contains Amlodipine 10mg, and Irbesartan 300mg in the form of TABLET, FILM COATED. It is approved for ORAL use.

This product is manufactured by SANOFI AVENTIS DE MEXICO S.A. DE C.V. in MEXICO.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Amlodipine is a long-acting 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, amlodipine prevents calcium-dependent myocyte contraction and vasoconstriction. A second proposed mechanism for the drug’s vasodilatory effects involves pH-dependent inhibition of calcium influx via inhibition of smooth muscle carbonic anhydrase. Some studies have shown that amlodipine also exerts inhibitory effects on voltage-gated N-type calcium channels. N-type calcium channels located in the central nervous system may be involved in nociceptive signaling and pain sensation. Amlodipine is used to treat hypertension and chronic stable angina.

Indication

For the treatment of hypertension and chronic stable angina.

Mechanism of Action

Amlodipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of amlodipine result in an overall decrease in blood pressure. Amlodipine is a long-acting CCB that may be used to treat mild to moderate essential hypertension and exertion-related angina (chronic stable angina). Another possible mechanism is that amlodipine inhibits vascular smooth muscle carbonic anhydrase I activity causing cellular pH increases which may be involved in regulating intracelluar calcium influx through calcium channels.

Pharmacokinetics

Absorption: Amlodipine is slowly and almost completely absorbed from the gastrointestinal tract. Peak plasma concentrations are reached 6-12 hour following oral administration. Its estimated bioavailability is 64-90%. Absorption is not affected by food.
Distribution
Metabolism: Hepatic. Metabolized extensively (90%) to inactive metabolites via the cytochrome P450 3A4 isozyme.
Elimination

Toxicity

Gross overdosage could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to an including shock with fatal outcome have been reported.

Active Ingredient/Synonyms

(RS)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate | 3-Ethyl 5-methylester, (±)-2-[(2-aminoethoxy)methyl]-4-(o-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate | 3-Ethyl-5-methyl (+-)-2-(2-aminoethoxymethyl)-4-(O-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate | Amlodipine | Amlodipine free base | Amlodipino | Amlodipinum | Amlodipine |

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

Description

Irbesartan is an angiotensin receptor blocker (ARB) used mainly for the treatment of hypertension. It competes with angiotensin II for binding at the AT1 receptor subtype. Unlike ACE inhibitors, ARBs do not have the adverse effect of dry cough. The use of ARBs is pending revision due to findings from several clinical trials suggesting that this class of drugs may be associated with a small increased risk of cancer.

Indication

For the treatment of hypertension, as well as diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension. Irbesartan is also used as a second line agent in the treatment of congestive heart failure.

Mechanism of Action

Irbesartan is a nonpeptide tetrazole derivative and an angiotensin II antagonist that selectively blocks the binding of angiotensin II to the AT₁ receptor. In the renin-angiotensin system, angiotensin I is converted by angiotensin-converting enzyme (ACE) to form angiotensin II. Angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle. Irbesartan, by blocking the binding of angiotensin II to the AT₁ receptor, promotes vasodilation and decreases the effects of aldosterone. The negative feedback regulation of angiotensin II on renin secretion is also inhibited, but the resulting rise in plasma renin concentrations and consequent rise in angiotensin II plasma concentrations do not counteract the blood pressure–lowering effect that occurs. The action of ARBs is different from ACE inhibitors, which block the conversion of angiotensin I to angiotensin II, meaning that the production of angiotensin II is not completely inhibited, as the hormone can be formed via other enzymes. Also, unlike ACE inhibitors, irbesartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough).

Pharmacokinetics

Absorption: Rapid and complete with an average absolute bioavailability of 60-80%. Food has no affect on bioavailability.
Distribution: * 53 to 93 L
Metabolism: Hepatic. Irbesartan is metabolized via glucuronide conjugation and oxidation. In vitro studies of irbesartan oxidation by cytochrome P450 isoenzymes indicated irbesartan was oxidized primarily by 2C9; metabolism by 3A4 was negligible.
Elimination

Clearance

* 157-176 mL/min

Toxicity

Hypotension and tachycardia; bradycardia might also occur from overdose, LD₅₀=mg/kg(orally in rat)

Active Ingredient/Synonyms

2-butyl-3-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1,3-diazaspiro[4.4]non-1-en-4-one | Irbesartan | Irbesartan |

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post APROVASC FILM COATED TABLET 300MG/10MG appeared first on Singapore Drugs Database.

COXETA FC TABLETS 60MG

Admin — Sun, 20 Jun 2021 16:25:33 +0000

Product Information

Registration Status: Active

Description

Indication

For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

Mechanism of Action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.

Pharmacokinetics

Absorption: Bioavailability is 100% following oral administration.
Distribution
Metabolism: Hepatic, primarily via CYP3A4.
Elimination

Toxicity

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post COXETA FC TABLETS 60MG appeared first on Singapore Drugs Database.

COXETA FC TABLETS 90MG

Admin — Sun, 20 Jun 2021 16:25:32 +0000

Product Information

Registration Status: Active

Description

Indication

For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

Mechanism of Action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.

Pharmacokinetics

Absorption: Bioavailability is 100% following oral administration.
Distribution
Metabolism: Hepatic, primarily via CYP3A4.
Elimination

Toxicity

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

The post COXETA FC TABLETS 90MG appeared first on Singapore Drugs Database.