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Venlafaxine
HCl API |
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Haorui supplies Venlafaxine HCl API (Active Pharmaceutical
Ingredients) to pharmaceutical industry. Our bulk
Venlafaxine HCl actives is produced by GMP facility.
Welcome to contact us for
product detail.
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The
following information is provided for general information
purposes ONLY.
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What
is Venlafaxine?
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Venlafaxine
is a phenethylamine bicyclic derivative, which is a
structurally novel antidepressant
for oral administration. It is chemically unrelated to
tricyclic, tetracyclic, or other available antidepressant
agents.
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What
is the advantage of Venlafaxine?
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Venlafaxine
seems to have the relative freedom from side-effects
associated with the SSRIs [fluoxetine (Prozac), sertraline
(Zoloft), paroxetine (Paxil), and fluvoxamine (Luvox)] and the
impact on both serotonin and norepinephrine associated with
the tricyclic antidepressants [amitriptyline (Elavil),
imipramine (Tofranil), etc.]. It is hypothesized that the
action of the venlafaxine molecule upon both serotonin and
norepinephrine will cause venlafaxine to be a successful
antidepressant for some people who have not responded to
treatment with SSRIs.
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As
venlafaxine and its active metabolite have relatively short
half-lives, 4 hours and 11 hours respectively, venlafaxine
should be administered in divided does, two or three times a
day.
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What
kinds of depression can be treated with venlafaxine?
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While
the pre-marketing studies were restricted to patients with a
DSM-III-R diagnosis of Major Depressive Disorder (with or
without melancholia), it is to be expected that venlafaxine
will be prescribed for patients with Major Depression,
Dysthymia, and Bipolar Disorder.
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While
venlafaxine was only studied for periods up to 6 weeks, it is
to expected that patients with long-standing depressions will
take the drug for longer periods of time.
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What is Venlafaxine chemical
formula? |
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It is designated (R/S)-1-[2-(dimethylamino)-1-(4
methoxyphenyl)ethyl] cyclohexanol hydrochloride or (±)-1-[a
[(dimethylamino)methyl] p-methoxybenzyl] cyclohexanol hydrochloride and has the empirical formula of C17H27NO2
HCl. Its molecular weight is 313.87 |
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What is Venlafaxine
appearance? |
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Venlafaxine hydrochloride is a white to off-white crystalline solid with a solubility of 572 mg/ml in water (adjusted to ionic strength of 0.2 M with sodium chloride). Its octanol:water (0.2 M sodium chloride) partition coefficient is 0.43. |
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What
is the mechanism of Venlafaxine?
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The
mechanism of venlafaxine's antidepressant action in humans is
believed to be associated with its potentiation of
neurotransmitter activity in the CNS. Preclinical studies have
shown that venlafaxine and its major metabolite, O-desmethylvenlafaxine
(ODV), are potent inhibitors of neuronal serotonin and
norepinephrine reuptake and weak inhibitors of dopamine
reuptake.
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Venlafaxine
and ODV have no significant affinity for muscarinic,
histaminergic, or alpha1-adrenergic receptors in vitro.
Pharmacologic activity at these receptors is hypothesized to
be associated with the various anticholinergic, sedative, and
cardiovascular effects seen with other psychotropic drugs.
Venlafaxine and ODV do not possess monoamine oxidase (MAO)
inhibitory activity. |
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What
is treated with venlafaxine other than depression?
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There
is accumulating evidence that the symptoms of ADD/ADHD in both
children and adults can be treated with venlafaxine. High
doses of venlafaxine have also been reported to be effective
in the treatment of people with borderline personality
disorder.
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Does other
medications interact with venlafaxine?
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Lithium - No interaction.
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Diazepam (Valium) - No
interaction.
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Cimetidine (Tagamet) - Slight
increase in blood level of venlafaxine's active metabolite.
Not of clinical significance.
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Fluoxetine
(Prozac) - Significant increase in the concentration of
venlafaxine and its active metabolite. Potential for increased
side-effects.
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Take
venlafaxine with alcohol?
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Although
venlafaxine has not been found to increase the impairment of
cognitive or motor skills caused by alcohol, the manufacturer
warns against drinking while taking venlafaxine.
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The
time venlafaxine takes to relieve depression
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While
most people taking venlafaxine become aware of some lessening
of depression within two to four weeks, there are some who
experience relief within the first week and others who only
experience relief after a couple of months of therapy.
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Venlafaxine
Pharmacokinetics
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Venlafaxine
is well absorbed, with peak plasma concentrations occurring
approximately 2 hours after dosing. Venlafaxine is extensively
metabolized, with O-desmethylvenlafaxine. Approximately 87% of
a single dose of venlafaxine is recovered in the urine within
48 hours as either unchanged venlafaxine (5%).
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Venlafaxine
Multiple-Dose Pharmacokinetic Profile
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Steady-state
concentrations of both venlafaxine and ODV in plasma were
attained after approximately 3 days of multiple dose therapy.
The clearance of venlafaxine is slightly (15%) lower following
multiple doses than following a single dose.
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Is
venlafaxine safe for a woman who is pregnant?
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There
is no data to establish the safety of venlafaxine for the
fetus or nursing infant.
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What
are the venlafaxine side-effects of?
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The
most common side-effects and the percentage of people
reporting them during clinical trials are: Nausea, Headache,
Sleepiness, Dry mouth, Dizziness, Insomnia, Constipation,
Nervousness, Raised blood pressure, Fatigue, Sweating,
Decreased appetite, Male sexual dysfunction, Female sexual
dysfunction.
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Disclaimer:
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Information
on this page is provided for general information purposes. You
should not make a clinical treatment decision based on
information contained in this page without consulting other
references including the package insert of the drug, textbooks
and where relevant, expert opinion. We cannot be held
responsible for any errors you make in administering drugs
mentioned on this page, nor for use of any erroneous
information contained on this page.
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