Telmisartan Use in Hypertension

Abstract: Telmisartan is used alone or in combination with other medications to treat high
blood pressure. Telmisartan is also used to decrease the chance of heart attack, stroke, or death
in people 55 years of age or older who are at high risk for cardiovascular disease. Telmisartan is
in a class of medications called angiotensin II receptor antagonists. It works by blocking the
action of certain natural substances that tighten the blood vessels, allowing the blood to flow
more smoothly and the heart to pump more efficiently.

Telmisartan is an angiotensin II receptor antagonist that is highly selective for type 1

angiotensin II receptors. It was significantly more effective than placebo in large (n
>100), double-blind, randomised, multicentre clinical trials in patients with mild to
moderate hypertension. Telmisartan 20 to 160mg once daily produced mean reductions
in supine trough systolic blood pressure and diastolic blood pressure of up to 15.5 and
10.5mm Hg, respectively. Maximum blood pressure reduction occurred with a dosage of
40 to 80 mg/day.
Telmisartan 40 to 120 mg/day was as effective as amlodipine 5 to 10 mg/day or atenolol
50 to 100 mg/day in dose-titration studies. Telmisartan 20 to 160 mg/day was generally
similar in efficacy to enalapril 5 to 20 mg/day or lisinopril 10 to 40 mg/day in both
titration-to-response and other studies. Hydrochlorothiazide was coadministered in
most of the titration-to-response studies if patients remained hypertensive.
Telmisartan 80 mg/day was more effective than submaximal dosages of losartan (50
mg/day) or valsartan (80 mg/day) and was as effective as a fixed-dose combination of
losartan 50mg plus hydrochlorothiazide 12.5mg over the last 6 hours of the dosage
interval and the whole 24-hour postdose interval. In patients with severe hypertension,
telmisartan 80 to 160 mg/day was as effective as enalapril 20 to 40 mg/day (both agents
could be titrated and combined sequentially with hydrochlorothiazide 25mg and
amlodipine 5mg).
The addition of hydrochlorothiazide to telmisartan was more effective than each agent
alone at lowering blood pressure in patients with hypertension.
Conclusion: Telmisartan is an effective antihypertensive agent with a tolerability profile
similar to that of placebo. Comparative data have shown telmisartan to be as effective
as other major classes of antihypertensive agents at lowering blood pressure. Compared
with lisinopril, telmisartan is associated with a significantly lower incidence of dry,
persistent cough. Therefore, telmisartan is a useful therapeutic option in the
management of patients with hypertension.

Receptor blocker-Several orally active non-peptide angiotensin II subtype

1 (AT1) receptor antagonists are now available for the treatment of
hypertension. These agents have a common mechanism of actionblockade of the binding of angiotensin II to the subtype 1 receptor - and
their binding to this receptor is generally insurmountable. There are some
pharmacokinetic and pharmacodynamic differences between these
antagonists, which may reflect in their clinical efficacy, especially at the
end of the dosing interval. Losartan has an active metabolite that prolongs
its duration of action, and candesartan cilexetil requires conversion to an
active form after administration. Telmisartan has the longest duration of
action, with a terminal elimination half-life of around 24 h in comparison
with 11-15 h for irbesartan, the agent with the next longest half-life. The
long duration of action and insurmountable binding to the receptor may
be related to the slow dissociation kinetics of the antagonists from the AT1
receptor. Comparative clinical studies suggest that at the recommended
dose losartan, the original drug in this class, has a lower efficacy than the
newer agents, such as telmisartan. It is possible that these differences
between angiotensin II receptor antagonists are due to variations in the
degree and duration of receptor blockade, and may be of clinical
significance with regard to the cardioprotective and renoprotective effects
of this class of antihypertensive agents.
Pharmacokinetics and PharmacodynamicsAs toxicology is a continuum of pharmacokinetics and pharmacodynamics,
this is a review of recent advances on pharmacokinetics and
physiologically-based pharmacokinetic (PBPK) modeling involving
nanoparticles. We provide a synopsis of the state-of-the-science on the
absorption, distribution, metabolism, and excretion
angiotensin II mediates its haemodynamic effects by binding to specific
cell-surface receptors. In humans, two receptor subtypes have been
identified, designated AT1 and AT2. Because all major deleterious effects of
angiotensin II are produced via binding to AT1-receptors, selective
blockade of this receptor subtype should confer haemodynamic benefits,
while allowing stimulation of the potentially beneficial effects mediated by
AT2-receptors. Experimental studies using various models have
consistently revealed marked differences in the receptor binding
properties of different AT1-receptor blockers. The relative receptor binding
affinities of currently available AT1-receptor blockers is candesartan >
irbesartan > valsartan/EXP-3174/telmisartan > tasosartan > losartan >
eprosartan. Candesartan is also released from the receptor more slowly
than other available AT1-receptor blockers, with a half-life of approximately
152 min for the receptor-blocker complex, compared with 31 min for EXP-

3174, 17 min for irbesartan and 5 min for losartan. Candesartan therefore
binds to the AT1-receptor more tightly and more persistently than other
AT1-receptor blockers.

Active Pharma Ingredients (API)

TELSARTAN TELMISARTAN

Cardiac

TELSARTAN-AM AMLODIPINE + OTHERS

Cardiac

TELSARTAN-H TELMISARTAN + HCT

Cardiac

TELSARTAN-R TELMISARTAN+RAMIPRIL

Cardiac

Dose response and safety of telmisartan in patients with mild to moderate hypertension
This randomized, double-blind, double-dummy, placebo-controlled, parallel-group
study evaluated the dose-response relationship of telmisartan in 207 patients
with mild to moderate hypertension (diastolic blood pressure [DBP] 100 to 114
mmHg). After a 28-day placebo run-in period, patients were randomized to 28
days of once-daily, double-blind, double-dummy treatment with telmisartan 40,
80, or 120 mg; enalapril 20 mg; or placebo. Blood pressure (BP) was manually
recorded for 12 hours after the first dose and after 24 hours at baseline (Day 0),
Day 1, and Day 28 of double-blind treatment. Pharmacokinetic and
pharmacodynamic parameters were assessed from telmisartan plasma
concentrations. All doses of telmisartan and enalapril significantly reduced BP
compared with placebo
BP reductions after 4 weeks of treatment with telmisartan were no different from
those achieved with enalapril. No significant linear trend in BP reduction was
evident among telmisartan doses. Reductions in SBP and DBP were maintained
over the 24-hour period at Day 28. Treatment did not affect supine heart rate.
Dosage Adult: PO Initial: 40 mg once daily. Max: 80 mg/day.
Administration May be taken with or without food.

Medial Serve for TELMISARTAN molecule Products on KARVE road medicals dated
22nov2011.
Dr. LIST ON KARVE ROAD
Dr.Nilesh Kulkarni

Dr.Sudhir Mundle

Dr.Anand Siya (MBBS)

Dr.Agrawal

Dr.Rane

Dr. Phatake

Dr. Shendgekar

Dr.Prathiba Phadke

Dr.A. Bapat

Dr.Javdekar

Dr. Bhatt

STOKISTNitin

Anand

Kundan

Tapdia

Prasad

Ravi

Maharashtra

Amar agencies

Arun

Shaha

MEDICAL ON KARVE ROAD

Sai Shradha Medical

Mahesh Medical

Pulse Medical

Ashwini Medical

Sanjay medical

Shriram Medical

New Bharti Medical

Reliff medical

Swami Vivekanand Medical

Varad Medical

Medicine Point

Pooja medicals

Maharashtra Medical

Chaitali Medical

JeevanJyoti Medical

Arihant chemist

Niaa aushadh Bazzar

Mayur Medical

Anish Medical

Medicare Chemist

Chintamani Medico

Regal Chemist

Metro Medical

Relif medical

Swaroop Medical

Religare Medical

Anand Medical

Varad Medical

Medi-Plus

Pooja drugs

Shankar Medical

MAIN COMPETATORS FOR TELSARTAN BRANDS

TELVAS

- ABBOTT

TELMIKIND - MANKIND
TELMA

- GLENMARK

TELISTA

- LUPIN

PRICE LIST TELSRTAN PRODUCT

TELSARTAN tab

Telmisartan 20mg

DR. REDDY'S LABS

15

51.75

TELSARTAN tab

Telmisartan 40mg

DR. REDDY'S LABS

15

109.50

Telmisartan 80mg

DR. REDDY'S LABS

10

119.00

DR. REDDY'S LABS

10

85.50

TELSARTAN-ATR Telmisartan 20mg, atorvastatin 10mg DR. REDDY'S LABS

10

90.00

TELSARTAN
tab

TELSARTAN-AM Telmisartan 40mg, amlodipine 5mg

tab

tab

TELSARTANTelmisartan 80mg,
H tab

DR. REDDY'S LABS

15

137.70

TELSARTANTelmisartan 40mg,
H tab

DR. REDDY'S LABS

10

124.80

TELSARTANTelmisartan 40mg, ramipril 2.5mg

R tab

DR. REDDY'S LABS

10

77.00

TELSARTANTelmisartan 40mg, ramipril 5mg

R tab

DR. REDDY'S LABS

10

102.00

hydrochlorothiazide 12.5mg

hydrochlorothiazide 12.5mg

Telma - Glenmark (Zoltan) [Telmisartan]

Strength
Telma 20mg
Telma 40mg
Telma 80mg

Volume
10
10
10

Presentation
Telma TAB
Telma TAB
Telma TAB

Price*
38.90
71.00
119.40

Volume Presentation

Price*

Telma- H - Glenmark (Zoltan) [Telmisartan]

Combination
Telma- H Telmisartan 40mg,
Hydrochlorothiazide
12.5mg

10 Telma- H TAB

Telma- R - Glenmark (Zoltan) [Telmisartan]

Combination
Telma- R Telmisartan 40mg,
Ramiroil 5mg
Telma- R Telmisartan 40mg,
Ramiroil 5mg

Volume Presentation
10 Telma- R TAB
10 Telma- R TAB

MONTHLY SALE TELMISARTAN MOLECULE STRIP PER

MONTH(approximately)
TELSARTAN

Dr.Reddys

220

Price*

TELMA

Glenmark

303

TELVAS

ABBOTT

58

NoteBlue -

Telma

Orange Telsartan
Green - Telvas
CONCLUSION

Rx status outside
Residential Dr. Not available
No scheme for product
Price is much more comparative to other main competators