Afentral
Afentral Uses, Dosage, Side Effects, Food Interaction and all others data.
The efficacy of Afentral is presumed to be linked to potentiation of serotonergic activity in the central nervous system resulting from inhibition of neuronal reuptake of serotonin (5-hydroxy-tryptamine, 5 HT). Studies at clinically relevant doses in humans have demonstrated that paroxetine blocks the uptake of serotonin into human platelets. In vitro studies in animals also suggest that paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. In vitro radioligand binding studies indicate that paroxetine has little affinity for muscarinic, alpha1, alpha2, beta adrenergic, dopamine (D2), 5-HT1, 5 HT2 and histamine (H1)-receptors; antagonism of muscarinic, histaminergic and alpha1-adrenergic receptors has been associated with various anticholinergic, sedative and cardiovascular effects for other psychotropic drugs. Because the relative potencies of paroxetine’s major metabolites are at most 1/50 of the parent compound, they are essentially inactive.
Afentral treats the symptoms of depression, various anxiety disorders, posttraumatic stress disorder, obsessive-compulsive disorder, and the vasomotor symptoms of menopause via the inhibition of serotonin reuptake. The onset of action of paroxetine is reported to be approximately 6 weeks.
Due its serotonergic activity, paroxetine, like other SSRI drugs, may potentiate serotonin syndrome. This risk is especially high when monoamine oxidase (MAO) inhibitors are given within 2 weeks of paroxetine administration. Upon cessation of MAO inhibitors, a 2-week interval before paroxetine administration is recommended. Do not coadminister these agents.
| Trade Name | Afentral |
| Availability | Prescription only |
| Generic | Paroxetine |
| Paroxetine Other Names | Paroxetina, Paroxetine, Paroxetinum |
| Related Drugs | Rexulti, sertraline, trazodone, escitalopram, fluoxetine, alprazolam, duloxetine, Lexapro, amitriptyline, venlafaxine |
| Type | |
| Formula | C19H20FNO3 |
| Weight | Average: 329.3654 Monoisotopic: 329.142721716 |
| Protein binding | Paroxetine is 95% bound to plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | SSRIs & related anti-depressant drugs |
| Manufacturer | |
| Available Country | Cyprus |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Afentral is used for:
- Major Depressive Disorder
- Obsessive Compulsive Disorder
- Panic Disorder
- Social Anxiety Disorder
- Generalized Anxiety Disorder
- Posttraumatic Stress Disorder.
Afentral is also used to associated treatment for these conditions: Generalized Anxiety Disorder (GAD), Irritable Bowel Syndrome (IBS), Major Depressive Disorder (MDD), Obsessive Compulsive Disorder (OCD), Panic Disorder, Post Traumatic Stress Disorder (PTSD), Premature Ejaculation, Premenstrual Dysphoric Disorder, Social Anxiety Disorder (SAD), Vasomotor Symptoms Associated With Menopause
How Afentral works
Afentral enhances serotonergic activity via the inhibition presynaptic reuptake of serotonin by the serotonin (SERT) receptor. This inhibition raises the level of serotonin in the synaptic cleft, relieving various symptoms. This drug has been demonstrated to be a stronger inhibitor of serotonin reuptake than other members of the same drug class, including Citalopram, Fluoxetine, and Fluvoxamine. The mechanism of action of paroxetine in relieving the vasomotor symptoms of menopause is unknown, according to the Brisdelle prescribing information, but may occur due to its effects on thermoregulation.
Afentral shows a clinically insignificant affinity for adrenergic alpha-1 and alpha-2 receptors and β-adrenergic receptors, dopamine D1 and D2 receptors, histamine H1 receptors and serotonin 5-HT1A, 5-HT2A and 5-HT2C receptors. This drug shows some affinity for muscarinic cholinergic receptors and 5-H2B receptors. The delayed onset of paroxetine therapeutic effects may be explained by the initial paroxetine actions on the 5-HT neurons. In rats, paroxetine activates 5-HT1A receptors when it is first administered, inhibiting the stimulation of the 5-HT neurons and subsequent release of serotonin at the synaptic cleft.
Dosage
Afentral dosage
Major Depressive Disorder:
- Usual Initial Dosage: Afentral (Afentral hydrochloride) should be administered as a single daily dose with or without food, usually in the morning. The recommended initial dose is 20 mg/day. Some patients not responding to a 20 mg dose may benefit from dose increases, in 10 mg/day increments, up to a maximum of 50 mg/day. Dose changes should occur at intervals of at least 1 week.
- Maintenance Therapy: Systematic evaluation of the efficacy of Afentral hydrochloride has shown that efficacy is maintained for periods of up to 1 year with doses that averaged about 30 mg.
Obsessive Compulsive Disorder (OCD):
- Usual Initial Dosage: Afentral (Afentral hydrochloride) should be administered as a single daily dose with or without food, usually in the morning. The recommended dose of Afentral in the treatment of OCD is 40 mg daily. Patients should be started on 20 mg/day and the dose can be increased in 10 mg/day increments. Dose changes should occur at intervals of at least 1 week.
- Maintenance Therapy: Dosage adjustments should be made to maintain the patient on the lowest effective dosage, and patients should be periodically reassessed to determine the need for continued treatment.
Panic Disorder:
- Usual Initial Dosage: Afentral should be administered as a single daily dose with or without food, usually in the morning. The target dose of Afentral in the treatment of panic disorder is 40 mg/day. Patients should be started on 10 mg/day. Dose changes should occur in 10 mg/day increments and at intervals of at least 1 week. The maximum dosage should not exceed 60 mg/day.
- Maintenance Therapy: Dosage adjustments should be made to maintain the patient on the lowest effective dosage, and patients should be periodically reassessed to determine the need for continued treatment.
Social Anxiety Disorder (SAD):
- Usual Initial Dosage: Afentral should be administered as a single daily dose with or without food, usually in the morning. The recommended initial dosage is 20 mg/day.
- Maintenance Therapy: Dosage adjustments should be made to maintain the patient on the lowest effective dosage, and patients should be periodically reassessed to determine the need for continued treatment.
Generalized Anxiety Disorder (GAD):
- Usual Initial Dosage: Afentral should be administered as a single daily dose with or without food, usually in the morning. The recommended starting dosage and the established effective dosage is 20 mg/day.
- Maintenance Therapy: Dosage adjustments should be made to maintain the patient on the lowest effective dosage, and patients should be periodically reassessed to determine the need for continued treatment.
Posttraumatic Stress Disorder (PTSD):
- Usual Initial Dosage: Afentral should be administered as a single daily dose with or without food, usually in the morning. The recommended starting dosage and the established effective dosage is 20 mg/day. Dose changes, if indicated, should occur in 10 mg/day increments and at intervals of at least 1 week.
- Maintenance Therapy: Dosage adjustments should be made to maintain the patient on the lowest effective dosage, and patients should be periodically reassessed to determine the need for continued treatment.
Side Effects
Major depressive disorder: Asthenia, sweating, nausea, decreased appetite, somnolence, dizziness, insomnia, tremor, nervousness, ejaculatory disturbance and other male genital disorders.
Obsessive compulsive disorder: Nausea, dry mouth, decreased appetite, constipation, dizziness, somnolence, tremor, sweating, impotence and abnormal ejaculation.
Panic disorder: Asthenia, sweating, decreased appetite, decreased libido , tremor, abnormal ejaculation, female genital disorders and impotence.
Social anxiety disorder: Sweating, nausea, dry mouth, constipation, decreased appetite, somnolence, tremor, decreased libido, yawn, abnormal ejaculation, female genital disorders and impotence.
Generalised anxiety disorder: Asthenia, infection, constipation, decreased appetite, dry mouth, nausea, decreased libido, somnolence, tremor, sweating and abnormalejaculation.
Post-traumatic stress disorder: Asthenia, sweating nausea, dry mouth, diarrhoea, decreased appetite, somnolence, decreased libido, abnormal ejaculation, female genital disorders and impotence.
Toxicity
The acute LD50 in mice and rats is 350 mg/kg.
Overdose information
The lowest dose of paroxetine reported to lead to a fatal outcome is approximately 400 mg. The largest reported paroxetine overdose from which a patient has survived and recovered is a dose of 2000 mg. Common manifestations in a paroxetine overdose include fatigue, fever, insomnia hypertension, tachycardia, nausea, vomiting, somnolence, tremor, dizziness, agitation, confusion, anxious symptoms, headache, insomnia, hyperhidrosis, dilated pupils, seizures, paresthesia, serotonin syndrome, involuntary muscle contraction, and change in mental status. It should be noted that in some cases, patients may have consumed alcohol in addition to taking an overdose of paroxetine. Some of these symptoms may also be seen with clinical use. There is no specific antidote to an overdose of paroxetine.
Precaution
Cardiac conditions: Afentral does not produce clinically significant changes in blood pressure, heart rate and ECG. Nevertheless, as with all psychoactive drugs, caution is advised when treating patients with cardiac conditions.
Epilepsy: As with other antidepressants, Afentral should be used with caution in-patients with epilepsy.
Seizures: Overall, the incidence of seizures is < 0.1% in patients treated with Afentral. Afentral should be discontinued in any patient who develops seizures.
ECT: There is little clinical experience of concurrent administration of Afentral with ECT.
Ability to drive/use machines: Clinical experience has shown that therapy with Afentral is not associated with impairment of cognitive or psychomotor function. However, as with all psychoactive drugs, patients should be cautioned about their ability to drive a car and operate machinery.
Discontinuation of Treatment with Afentral: Recent clinical trials supporting the various approved indications of Afentral employed a taper phase regimen, rather than an abrupt discontinuation of treatment. The taper phase regimen used in GAD and PTSD clinical trials involved an incremental decrease in the daily dose by 10 mg/day at weekly intervals. When a daily dose of 20 mg/day was reached, patients were continued on this dose for 1 week before treatment was stopped.
Interaction
Food/antacids: The absorption and pharmacokinetics of Afentral are not affected by food or antacids.
Tryptophan: As with other 5-HT re uptake inhibitors, animal studies indicate that an interaction between Afentral and Tryptophan may occur, resulting in a ‘serotonin syndrome’ suggested by a combination of agitation, restlessness and gastrointestinal symptoms including diarrhoea.
Drug metabolizing enzyme inducers /inhibitors: The metabolism and pharmacokinetics of Afentral may be affected by drugs, which induce or inhibit hepatic drug metabolizing enzymes. When Afentral is to be coadministered with a known drug metabolizing inhibitor, consideration should be given to using doses at the lower end of the range. No initial dosage adjustment of Afentral is considered necessary when it is to be co-administered with known drug metabolizing enzyme inducers. Any subsequent dosage adjustment should be guided by clinical effect (tolerabilityand efficacy).
Alcohol: Although Afentral does not increase the impairment of mental and motor skill caused by alcohol, the concomitant use of Afentral and alcohol in depressed patients is not advised.
Haloperidol/amylobarbitone/oxazepam: Experience in a limited number of healthy subjects has shown that Afentral did not increase the sedation and drowsiness associated with haloperidol, amylobarbitone or oxazepam when given in combination.
MAOls: As with other 5-HT re uptake inhibitors, animal studies indicate that an interaction between Afentral and monoamine oxidase (MAO) inhibitors may occur.
Lithium: Since there is little clinical experience, and there have been reports of interaction of lithium with other 5-HT re-uptake inhibitors, the concurrent administration of Afentral and lithium should be undertaken with caution.
Lithium levels should be monitored. Phenytoin / anticonvulsants: Co-administration of Afentral and phenytoin is associated with decreased plasma concentrations of Afentral and increased adverse experiences. Co-administration of Afentral with other anticonvulsants may also be associated with an increased incidence of adverse experiences.
Warfarin: Preliminary data suggest that there may be a pharmacodynamic interaction between Afentral and warfarin, which may result in increased bleeding in the presence of unaltered prothrombin times. Afentral should therefore be administered with great caution to patients receiving oral anticoagulants.
Food Interaction
- Avoid alcohol.
- Take with or without food. Food does not significantly affect absorption.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Afentral Drug Interaction
Moderate: aspirin, aspirin, pregabalin, metoprolol, metoprolol, acetaminophen / hydrocodone, quetiapine, alprazolam, cetirizineUnknown: fluticasone / salmeterol, omega-3 polyunsaturated fatty acids, atorvastatin, esomeprazole, albuterol, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, ergocalciferol, cholecalciferol
Afentral Disease Interaction
Major: depressionModerate: bone fractures, renal dysfunction, hyponatremia, glaucoma, liver disease, mania, platelet function, seizure disorders, SIADHMinor: weight loss
Volume of Distribution
Afentral has a large volume of distribution and is found throughout the body, including in the central nervous system. Only 1% of the drug is found in the plasma. Afentral is found in the breast milk at concentrations similar to the concentrations found in plasma.
Elimination Route
Afentral is readily absorbed from the gastrointestinal tract. Due to the first-pass metabolism, the bioavailability ranges from 30-60%. Cmax is attained 2 to 8 hours after an oral dose. Mean Tmax is 4.3 hours in healthy patients. The steady-state concentration of paroxetine is achieved within 7 to 14 days of oral therapy. In a pharmacokinetic study, AUC in healthy patients was 574 ng·h/mL and 1053 ng·h/mL in those with moderate renal impairment.
Half Life
The mean elimination half-life of paroxetine is about 21 hours. In healthy young subjects, mean elimination half-life was found to be 17.3 hours.
Clearance
The apparent oral clearance of paroxetine is 167 L/h. The clearance of paroxetine in patients with renal failure is significantly lower and dose adjustment may be required, despite the fact that it is mainly cleared by the liver. Dose adjustments may be required in hepatic impairment.
Elimination Route
About 2/3 of a single paroxetine dose is found to be excreted in the urine and the remainder is found to be excreted in feces. Almost all of the dose is eliminated as metabolites; 3% is found to be excreted as unchanged paroxetine. About 64% of a 30 mg oral dose was found excreted in the urine, with 2% as the parent drug and 62% appearing as metabolites. Approximately 36% of the dose was found to be eliminated in the feces primarily as metabolites and less than 1% as the parent compound.
Pregnancy & Breastfeeding use
This drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Labor and Delivery: The effect of Afentral on labor and delivery in humans is unknown.
Nursing Mothers: Like many other drugs, Afentral is secreted in human milk, and caution should be exercised when Afentral hydrochloride is administered to a nursing woman.
Contraindication
Concomitant use in patients taking either monoamine oxidase inhibitors (MAOIs) or thioridazine is contraindicated. This is contraindicated in patients with a hypersensitivity to Afentral.
Special Warning
Dosage for Elderly or Debilitated, and Patients with Severe Renal or Hepatic Impairment: The recommended initial dose is 10 mg/day for elderly patients, debilitated patients, and/or patients with severe renal or hepatic impairment. Increases may be made if indicated. Dosage should not exceed 40 mg/day.
Storage Condition
Keep out of the reach of children. Store at a cool and dry place. Protect from light and moisture.
Innovators Monograph
You find simplified version here Afentral
Afentral contains Paroxetine see full prescribing information from innovator Afentral Monograph, Afentral MSDS, Afentral FDA label
FAQ
What is Afentral used for?
Afentral often used to treat depression and also sometimes for obsessive compulsive disorder (OCD), panic attacks, anxiety or post-traumatic stress disorder (PTSD).Afentral is a type of antidepressant known as an SSRI (selective serotonin reuptake inhibitor).
Is Afentral a strong antidepressant?
Afentral is the most potent inhibitor of the reuptake of serotonin of all selective serotonin reuptake inhibitors (SSRIs) and has been studied in many randomised controlled trials (RCTs).
Is Afentral good for anxiety?
Afentral is an antidepressant medication approved for the treatment of generalized anxiety disorder (GAD) and other anxiety disorders. It is in the same class as Prozac and Zoloft. Like other selective serotonin reuptake inhibitors (SSRIs), it was developed as a treatment for depression.
What are the most common side effects of Afentral?
Nausea, drowsiness, dizziness, trouble sleeping, loss of appetite, weakness, dry mouth, sweating, blurred vision, and yawning may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Can Afentral cause weight gain?
Afentral associated with weight loss at first, long-term use of SSRIs is mostly linked to weight gain. Long-term use is considered treatment that lasts longer than six months. Of the SSRIs listed above, Afentral is most commonly associated with weight gain with both long-term and short-term use.
Does Afentral work immediately?
Afentral will not work immediately to help reduce your symptoms of panic disorder. Improvements are typically noticed within several days to weeks of starting your prescription, but it can be several months before you experience the full benefits of Afentral.
Does Afentral cause hair loss?
Some people who take medications for depression and mood stabilization may experience hair loss. Drugs that may cause this include: Afentral hydrochloride sertraline.
Is long term use of Afentral safe?
There are no known problems associated with long term use of Afentral. It is a safe and effective medication when used as directed.
Is Afentral bad for my liver?
Afentral therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.
Can I drink alcohol with Afentral?
Alcohol can increase the nervous system side effects of Afentral such as dizziness, drowsiness, and difficulty concentrating. Some people may also experience impairment in thinking and judgment. You should avoid or limit the use of alcohol while being treated with Afentral.
Is Afentral a sedative?
The side-effect profile of Afentralis largely similar to that of the other SSRIs, although Afentral tends to be more sedating and constipating in some patients, perhaps due to its anticholinergic activity.
Is Afentral a controlled substance?
Afentral is not a controlled substance under the Controlled Substances Act (CSA).
Does Afentral help to sleep?
In addition to reducing the number of night time awakenings attributed to VMS, Afentral 7.5 mg significantly increased the duration of sleep per night, indicating a link between reduced night time awakenings and improvement in overall sleep duration.
What does Afentral do to my brain?
It works by helping to restore the balance of a certain natural substance (serotonin) in the brain. Afentral is known as a selective serotonin reuptake inhibitor (SSRI). This medication may improve your mood, sleep, appetite, and energy level and may help restore your interest in daily living.
Is Afentral an antipsychotic?
Afentral is an antidepressant that belongs to group of drugs called selective serotonin reuptake inhibitors (SSRIs). Afentral affects chemicals in the brain that may be unbalanced in people with depression, anxiety, or other disorders.
How does Afentral make me feel?
Antidepressants like Afentral help to jump start your mood so you feel better. You may notice that you sleep better and get on with people more easily because you're less anxious. You will hopefully take little things that used to worry you in your stride.
Can Afentral cause high blood pressure?
The only antidepressants that don't cause high blood pressure as a side effect are selective-serotonin reuptake inhibitors (SSRIs) such as sertraline, citalopram, fluoxetine, and Afentral. So, make sure the doctor prescribing your mental health medications knows if you have hypertension
What happens when I stop taking Afentral?
Stopping Afentral abruptly may result in one or more of the following withdrawal symptoms: irritability, nausea, feeling dizzy, vomiting, nightmares, headache, and/or paresthesias (prickling, tingling sensation on the skin). Depression is also a part of bipolar illness
Is Afentral hard to get off of?
For most people who take Afentral, the drug, at some point, becomes ineffective. Getting off of an SSRI like Afentral isn't nearly as challenging as recovering from recreational drug use. Symptoms are usually mild and are easily managed by gradually decreasing the dose
Does Afentral affect memory?
These findings suggest that long-term treatment with Afentral is associated with improvement of verbal declarative memory deficits and an increase in hippocampal volume in PTSD.
Does Afentral cause dementia?
Compared with no antidepressant use, Afentral was associated with an increased risk of dementia with any exposure.
What is the best time to take Afentral?
Take Afentral once a day, in the morning. It's best to take it with food so it doesn't upset your stomach. Afentral tablets come in different strengths ranging from 10mg to 30mg.
What happens if I suddenly stop taking Afentral?
Missing doses of Afentral may increase your risk for relapse in your symptoms. Stopping Afentral abruptly may result in one or more of the following withdrawal symptoms: irritability, nausea, feeling dizzy, vomiting, nightmares, headache, and/or paresthesias (prickling, tingling sensation on the skin).
Does Afentral make me last longer in bed?
Afentral had better ability to delay ejaculation than placebo at the end of 12 weeks of treatment.
What are the long term effects of taking Afentral?
The most common adverse events reported during long-term treatment with Afentral were somnolence, nausea, headache, and sweating. Pharmacokinetic analysis showed no clear correlation between the concentrations of Afentral in plasma and either clinical efficacy or tolerability.
Can I drive after taking Afentral?
Do not drive or ride a bike just after you start taking Afentral. Taking Afentral may affect your ability to do things like driving a car, riding a bike, using machines, or anything else that needs a lot of focus. You might find it difficult to concentrate, you might feel sleepy and your eyesight may be blurred.
How long does it take to get used to Afentral?
It usually takes between 4 and 6 weeks before you feel the full benefits. Do not stop taking Afentral after a week or two just because you feel it is not helping your symptoms. Give the medicine at least 6 weeks to work.
How long can I stay on Afentral?
Treatments and self-care. A doctor will likely suggest that a person gradually tapers their dosage of Afentral. Tapering typically lasts for 4 weeks, but for Afentral, a doctor may suggest tapering the medication over 6–8 weeks to reduce the risk of symptoms.
Is Afentral safe during pregnancy?
Afentral use during pregnancy should be avoided because of the increased risk of cardiovascular defects in infants, regardless of whether they are categorized as minor, moderate, or severe.
Is it safe to take Afentral while breastfeeding?
Most authoritative reviewers consider Afentral one of the preferred antidepressants during breastfeeding. [1-7] Occasional mild side effects such as insomnia, restlessness and increased crying have been reported in breastfed infants.
