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Protriptyline; Uses, Side Effects, Interactions, Pregnancy

Protriptyline is a tricyclic antidepressant that was previously widely used in the therapy of major depression. Most of the tricyclic antidepressants have been shown to cause a low rate of mild and transient serum enzyme elevations and rare cases of clinically apparent acute cholestatic liver injury. The potential hepatotoxicity specifically of protriptyline, however, has not been well defined.

Protriptyline hydrochloride is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, protriptyline does not affect mood or arousal but may cause sedation. In depressed individuals, protriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission.

Mechanism of Action of Protriptyline

Protriptyline acts by decreasing the reuptake of norepinephrine and serotonin (5-HT). Protriptyline is a tricyclic antidepressant. It was thought that tricyclic antidepressants work by inhibiting the reuptake of the neurotransmitters norepinephrine and serotonin by nerve cells. However, this response occurs immediately, yet mood does not lift for approximately two weeks. It is now thought that changes occur in receptor sensitivity in the cerebral cortex and hippocampus. The hippocampus is part of the limbic system, a part of the brain involved in emotions. Presynaptic receptors are affected: α₁ and β₁ receptors are sensitized, α₂ receptors are desensitized (leading to increased noradrenaline production). Tricyclics are also known as effective analgesics for different types of pain, especially neuropathic or neuralgic pain. A precise mechanism for their analgesic action is unknown, but it is thought that they modulate anti-pain opioid systems in the CNS via an indirect serotonergic route. They are also effective in migraine prophylaxis, but not in abortion of acute migraine attack. The mechanism of their anti-migraine action is also thought to be serotonergic.

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Indications of Protriptyline

Contra Indications of Protriptyline

overactive thyroid gland
Disorder of Mental Processes due to a Brain Disease
Schizophrenia
Manic-Depression
Having Thoughts of Suicide
alcoholism
Increased Pressure in the Eye
closed angle glaucoma
heart attack within the last 30 days
abnormal heart rhythm
abnormally low blood pressure
asthma
gastroesophageal reflux disease
Hiatal Hernia
liver problems
Enlarged Prostate
Electroshock Therapy
recent operation
seizures
Cannot Empty Bladder
chronic idiopathic constipation

Dosage of protriptyline

Strengths: 5 mg; 10 mg

Depression

15 to 40 mg orally per day divided into three or four doses
Maximum dose: 60 mg/day

Geriatric Dose for Depression

5 mg orally 3 times a day, increasing gradually if necessary

Side Effects of protriptyline

The most common

nausea, vomiting, loss of appetite;
anxiety, sleep problems (insomnia);
dry mouth, unusual taste;
little or no urinating;
constipation;
vision changes;
breast swelling (in men or women); or
decreased sex drive, impotence, or difficulty having an orgasm.
blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
restless muscle movements in your eyes, tongue, jaw, or neck;
a light-headed feeling, like you, might pass out;
seizure (convulsions);
new or worsening chest pain, pounding heartbeats or fluttering in your chest;
sudden numbness or weakness, problems with vision, speech, or balance;
fever, sore throat, easy bruising, unusual bleeding;
painful or difficult urination;

Common

Abdominal or stomach pain
agitation
black, tarry stools
bleeding gums
blood in urine or stools
blurred vision
burning, crawling, itching, numbness, prickling, “pins and needles”, or tingling feelings
change in consciousness
changes in patterns and rhythms of speech
chest pain or discomfort
cold sweats
coma
confusion

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Rare

Abdominal or stomach pain
agitation or irritability
blurred vision
change in urination
chest pain or discomfort
confusion about identity, place, and time
convulsions
cool, pale skin
dizziness, faintness, or lightheadedness when getting up suddenly from a lying or
Anxiety
change in vision
seizures
weight loss
chest pain or tightness
confusion
cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
hallucinations
headache
irritability
muscle pain or cramps
pale or yellowed skin, dark colored urine, fever, confusion or weakness;
sore throat, and headache with a severe blistering, peeling, and red skin rash;
swelling, rapid weight gain, feeling short of breath (even with mild exertion); or
increased thirst , loss of appetite, urinating less than usual or not at all.

Drug Interaction of Protriptyline

Protriptyline may interact with following drugs, or suppliment & change thr efficacy of drugs

monoamine oxidase (MAO) inhibitors such as isocarboxazid, phenelzine selegiline , and tranylcypromine
amiodarone
antihistamines;
bupropion
celecoxib
cimetidine
ipratropium
medications for
medications for irregular heartbeat such as , moricizine and propafenone
other antidepressants
ranitidine
selective serotonin reuptake inhibitors (SSRIs) such as citalopram, fluoxetine , fluvoxamine , paroxetine and sertraline
sedatives or sleeping pills
thyroid medications
tramadol

This is not a complete list of protriptyline drug interactions. Ask your doctor or pharmacist for more information.

Pregnancy & Lactation of protriptyline

FDA Pregnancy catagory C

Pregnancy

Protriptyline has not been classified into one of these categories because safe use in pregnancy has not been established. The use of protriptyline in pregnant women or women who may become pregnant requires that possible benefits be weighed against possible hazards to the mother and child.

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Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. Safe use of protriptyline during breastfeeding has not been established. The use of protriptyline in nursing women requires that possible benefits be weighed against possible hazards to the mother and child.