Brand Information

Strength	Rate	Packing Style
2mg er caps	155.00	10s e.r caps
4mg er caps	310.00	10s er caps

Drug Interaction:

CYP3A4 inhibitors- ketoconazole an inhibitor of the drug metabolizing enzyme CYP3A4 significantly increased plasma concentrations of toterodine when coadministered to subjects who are poor metabolizers.

For patients receiving ketoconazole or other potent CYP3A4 inhibitors, such as azole antifungals eg. itraconazole, miconazole, or microlide e.g. erythromycin, clarithromycin, or cyclosporine or vanblastine, the recommended dose is 1mg twice daily

Fluoxetine- is a selective serotin uptake inhibitor (SSRI) and a potent inhibitor of cytochrome P450 2D6 activity. Fluoxetine significantly inhibited the metabolism of immediate release toterodine in extensive metabolisers.However, no dosage is required when tolterodine and fluoxetine are coadministered

Indication:

Tolerodine Tartrate Extended Release Tablets 2mg/4mg

Indication-

Treatment of Overactive Bladder-

(Approved by FDA on 31-01014( Ref- FDA approved List- 2014)

LIST OF DRUGS DURING 2007

Sr.No- 91

Name of the Drug- Tolterodine tartrate ER 4mg +

Tamsulocin Hcl ER 0.4mg tablet Pharmacological Classification- For BPH with overactive bladder

Date of Approval- 15-06-07

Approved by U.S.FDA on 30-12-2007 (Ref- FDA approved List- 2007)

LIST OF DRUGS DURING 2007

Sr.No- 98

Name of the Drug- Tolterodine tartrate ER 4mg +

Tamsulocin Hcl ER 0.4mg Capsule Pharmacological Classification- For BPH with overactive bladder

in Adults only

Date of Approval- 15-06-07

Approved by U.S.FDA on 30-12-2007 (Ref- FDA approved List- 2007)

New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing

(Ref- IDMA Publication)

Name of Drug Indication Date of Approval

1.Tolerodine tartarate 4mg 15-06-2007

+ Tamsulocin Hcl ER 0.4mg tablet

For BPH with Overactive Bladder

2.Tolterodone Tartarate Extended 31-01-2014

Release Tablets 2mg/4mg

Addl.Dosage Form

For the treatment of Overactive Bladder with symptoms of urge

Urinary Incontinence,Urinary Incontinence, Urgency and frequency

3.Tolterodone L-Tartarate 13-09-2001

Overactive bladder

FIXED DOSE COMBINATIONS APPROVED BY DCG(I)

FROM JANUARY 1961 TILL NOVEMBER 2014

Name of Drug Indication Date of Approval

Tolerodine Tartrate 4mg ER + 15-06-2007

Tamsulosin HCL 0.4mg capsule

For BPH with overactive bladder in adults

Overactive bladder -

Treatment of patients with overactive bladder with symptoms of urinary

incontinence, urgency, frequency

Adverse Reaction:

Vertigo/ dizziness

Dermatologic- dry skin,

GI - abdominal pain, constipation, diarrhea, dyspepsia,

GU- dysuria Metabolic / nutritional - weight gain

Musculoskeletal- arthalgia Special senses- xerophthalmia

Miscellaneous- fatigue, headache, infection, influenza like symptoms

Contra-Indications:

Urinary retension, gastric retension, or uncontrolled narrow angle glaucoma, hypersensitivity to th drug or its ingredients

Special precautions-

Risk of urinary retension and gstric retention- Administer with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention and to patients with GI obstructive disorders such as pyloric stenosis, because of risk of gastric retention.

Controlled narrow angle glacoma- Use toterodine with caution in patients being treated with narrow angle glaucoma

Pregnancy- Use tolterodine during pregnancy only if potential benefits for the mother justifies risk to the fetus.

Lactation- Do not administer tolterodine during nursing. Decide to discontinue nursing or discontiue tolterodine to nursing mothers.

Dosages/ Overdosage Etc:

Tolerodine Tartrate Extended Release Tablets 2mg/4mg

Indication-

Overactive bladder - Treatment of patients with overactive bladder with symptoms of urinary incontinence, urgency, frequency

Usual dosage- 2mg twice daily Dosage adjustment - lower the dose to 1mg twice daily based on individual response and tolerability

Renal function imparement- patients with significantly reduced renal function- recommended dose is 2mg daily for extended release capsules or 1mg twice daily for immediate release capsules

Hepatic function impairment- patients with significantly reduced hepatic function- recommended dose is 2mg daily for extended release capsules or 1mg twice daily for immediate release capsules

Patient Information:

Extended release tablets should be taken once daily with liquids and swallowed whole Inform patients that antimuscranic agents such as toleridine may produce blurred vision, dizziness, or drowsiness

Pharmacology/ Pharmacokinetics:

Ref - Drug Facts and Comparisons(2010)

Pharmacology-

Tolerodine is a competetive muscarinic receptor antagonist. Both urinary contraction and

salivation are mediated via cholinergic muscranic receptors

After oral admin. tolterodine is metabolised in the liver resulting in the formation of 5-hydroxymethyl derivative , a major pharmacologically active metabolite. This active metabolite which exhibits an antimusccarinic acttivity similar to tolterodine, contributes significantly to the therapeutic effect.

Pharmacokinetics-

Immediate release tolterodine is rapdily absorbed and maximum serum concentration Cmax typically occur within 1 to 2 hours after dose admin.

Food increases the bioavalability of toterodine ( average increase 53%) but does not affect the levels of 5-hydroxymethyl metabolite in extensive metabolizers. The change is not expected to be a safety concern and asdjustment of dose is not needed.

A summary of mean (standard deviation ) pharmacokinetic parameters of immediate release tolerodine and the 5-hydroxymethyl metabolite in extensive metabolisers(EM)and poor merabolizers (PM) is provided in the following table.

These data were obtained following single and multiple doses of 4mg tolerodine administered twice daily to 16 healthy male volunteers (8 extensive metabolisrs(EM) and

8 poor metabolizers (PM)

A summary of mean(+/- ) Pharmacokentic Parameters of

Tolerodine and its Active Metabolite (5-hydroxymethyl

Metabolite) in Healthy Volunteers

Tolterodine 5-hydroxymethyl

metabolite

Phenotype tmax Cmax Cavg t 1/2 CL/F tmax Cmax Cavg t 1/2

(CYP2D6) (hr) (mcg/L (mcg/L) (hr) (L/hr) (hr) (mcg/L (mcg/L) (hr)

Single dose

EM 1.6+/- 1.6+/- 0.5+/- 2+/- 534+/- 1.8+/- 1.8+/- 0.62+/- 3.1+/-

1.5 1.2 0.35 0.7 697 1.4 0.7 0.26 0.7

PM 1.4+/- 10+/- 8.3+/- 6.5+/- 17+/- NA NA NA NA

0.5 4.9 4.3 1.6 7.3

Multiple Dose

EM 1.2+/- 2.6+/- 0.58+/- 2.2+/- 415+/- 1.2+/- 2.4+/- 0.92+/- 2.9+/-

0.5 2.8 0.54 0.4 377 0.5 1.3 0.46 0.4

PM 1.9+/- 19+/- 12+/- 9.6+/- 11+/- NA NA NA NA

1 7.5 5.1 1.5 4.2

Interaction with Food:

Food increases the bioavailability of tolterodine about 53%

Pregnancy and lactation:

Pregnancy- Use tolterodine during pregnancy only if potential benefits for the mother justifies risk to the fetus.

Lactation- Do not administer tolterodine during nursing. Decide to discontinue nursing or discontiue tolterodine to nursing mothers.

ROLITEN

Drug Interaction

Indication

Adverse Reaction

Contra-Indications

Dosages/ Overdosage Etc

Patient Information

Pharmacology/ Pharmacokinetics

Interaction with Food

Pregnancy and lactation