Alprazolam History, Action, best Uses, Side effects, Dosage, & 30 Brands

Introduction

Alprazolam is a medication that belongs to the class of drugs known as benzodiazepines. It is commonly prescribed to treat anxiety and panic disorders. Alprazolam is known by its brand name Xanax and is widely recognized for its calming and sedative effects. It is considered a central nervous system (CNS) depressant, meaning it slows down brain activity.

History of Alprazolam

Alprazolam, commonly known by its brand name Xanax, is a medication that was developed in the late 1960s and early 1970s. It falls under the category of benzodiazepines, a class of drugs known for their calming and anxiety-relieving effects.

Development and Patents

Alprazolam was developed by J.B. Hester of Upjohn Laboratories (now part of Pfizer) in the late 1960s. Research on benzodiazepines led to the creation of alprazolam. The drug received a German patent in 1970, and a corresponding U.S. patent was issued in 1976.

FDA Approval and Release

The U.S. Food and Drug Administration (FDA) approved Xanax (alprazolam) on October 16, 1981. It was specifically approved for the treatment of anxiety and panic disorders. Xanax was the first medication to receive FDA approval specifically for panic attacks.

Popularity and Abuse

Following its release, Xanax quickly gained popularity and became the most widely prescribed benzodiazepine in the United States. However, it is important to note that Xanax is also widely abused. Due to its potential for misuse, the FDA classified it as a Schedule IV Controlled Substance, indicating a low risk of abuse and dependence.

Alprazolam Mechanism of action

Alprazolam, a benzodiazepine, works by enhancing the effect of a neurotransmitter called gamma-aminobutyric acid (GABA) in the brain. GABA is an inhibitory neurotransmitter, which means it helps to slow down or calm down brain activity.

Here’s a step-by-step explanation of how Alprazolam works:

1. GABA Binding: GABA binds to its receptors in the brain, which slows down the activity of neurons (nerve cells).
2. Alprazolam Binding: It binds to a specific site on the GABA receptor, known as the benzodiazepine receptor.
3. Enhanced GABA Effect: Alprazolam enhances the effect of GABA, allowing it to bind more effectively to its receptors.
4. Increased Inhibition: With Alprazolam, GABA’s inhibitory effect on neurons is increased, leading to a calming effect on the brain.
5. Reduced Anxiety: The increased inhibition of neurons reduces anxiety, panic, and stress responses.
6. Muscle Relaxation: It also has a muscle relaxant effect, which can help with anxiety-related muscle tension.
7. Sedation: At higher doses, Alprazolam can produce sedation, which can help with insomnia related to anxiety.

By enhancing the effect of GABA, Alprazolam helps to calm down the brain’s activity, reducing anxiety, panic, and stress responses. This makes it an effective treatment for anxiety disorders and panic disorders.

Alprazolam uses

Alprazolam, a benzodiazepine, is primarily used to treat anxiety and panic disorders. Here are some of the important uses of Alprazolam:

1. Anxiety Disorders: Alprazolam is effective in treating generalized anxiety disorder (GAD), social anxiety disorder, and specific phobias.
2. Panic Disorder: It is used to treat panic attacks and panic disorder, reducing the frequency and severity of attacks.
3. Seizures: It is sometimes used to treat seizures, particularly in people with epilepsy.
4. Muscle Spasms: Alprazolam has a muscle relaxant effect, making it useful for treating muscle spasms and cramps.
5. Chemotherapy-Induced Nausea: It help alleviate nausea and vomiting associated with chemotherapy.
6. Pre-Procedural Anxiety: This medicne can be used to calm patients before medical procedures, reducing anxiety and stress.
7. Social Anxiety Disorder: Alprazolam can help individuals with social anxiety disorder feel more comfortable in social situations.
8. Short-Term Anxiety Relief: It also provide quick relief from anxiety symptoms, making it a useful option for short-term use.

Alprazolam for sleep

Alprazolam, commonly known as Xanax, is sometimes prescribed off-label for insomnia or sleep difficulties, particularly when related to anxiety or stress. However, it’s important to note that Alprazolam is not a primary treatment for insomnia, and its use for sleep should be approached with caution. When used for sleep, Alprazolam can help individuals fall asleep faster and stay asleep longer.

Alprazolam Dosage

Alprazolam dosage varies depending on the condition being treated, age, and individual response. Always follow your doctor’s instructions and consult with them before making any changes. Here are general dosage guidelines:

For Anxiety Disorders

• Initial dose: 0.25-0.5 mg (milligrams) orally, 2-3 times a day
• Maintenance dose: 0.5-4 mg per day, divided into 2-3 doses

For Panic Disorder

• Initial dose: 0.5 mg orally, 2-3 times a day
• Maintenance dose: 1-10 mg per day, divided into 2-3 doses

For Insomnia

• Initial dose: 0.25-0.5 mg orally, once at bedtime
• Maintenance dose: 0.5-2 mg per day, once at bedtime

For Seizures

• Initial dose: 0.5-1 mg orally, 2-3 times a day
• Maintenance dose: 1-6 mg per day, divided into 2-3 doses

Elderly or Debilitated Patients

• Initial dose: 0.25 mg orally, 2-3 times a day
• Maintenance dose: 0.5-2 mg per day, divided into 2-3 doses

Maximum Daily Dose

• 4 mg per day for anxiety disorders and insomnia
• 10 mg per day for panic disorder

Dosage Adjustment

• Gradually increase the dose every 3-4 days as needed and tolerated
• Reduce the dose gradually when discontinuing the medication

Alprazolam Side effects

Alprazolam, like other benzodiazepines, can cause a range of side effects, some of which can be serious. It’s essential to be aware of these potential side effects and discuss any concerns with your doctor.

Common Side Effects

1. Drowsiness: It can cause drowsiness, especially during the initial stages of treatment.
2. Fatigue: Feeling tired or lethargic is a common side effect.
3. Memory Problems: Alprazolam can impair short-term memory and cognitive function.
4. Confusion: Some people may experience confusion or disorientation.
5. Dizziness: It can cause dizziness or lightheadedness, especially when standing up.
6. Increased Salivation: Some individuals may experience increased salivation.
7. Diarrhea: It also cause gastrointestinal issues like diarrhea.
8. Nausea: Nausea and vomiting are possible side effects.
9. Headache: Some people may experience headaches.
10. Muscle Weakness: It also cause muscle weakness or fatigue.

Less Common but Serious Side Effects

1. Allergic Reactions: Rare but potentially life-threatening allergic reactions can occur.
2. Seizures: It can increase the risk of seizures, especially in people with a history of seizure disorders.
3. Suicidal Thoughts: In rare cases, it can increase the risk of suicidal thoughts or behavior.
4. Dependence and Withdrawal: Alprazolam can be habit-forming, and sudden withdrawal can lead to serious side effects.
5. Liver Damage: Long-term use of Alprazolam can lead to liver damage or abnormal liver function tests.
6. Blood Disorders: It can cause blood disorders like agranulocytosis or thrombocytopenia.
7. Yellowing of the Skin and Eyes: Jaundice can occur in rare cases.
8. Pregnancy and Breastfeeding: It can harmful to the fetus or baby, and its use during pregnancy or breastfeeding should be discussed with a doctor.

Alprazolam (Xanax) vs Bromazepam (Lexotanil)

Similarities

Differences

• Alprazolam: Short-acting (4-6 hours)
• bromazepam: Intermediate-acting (8-12 hours)

• Alprazolam: More potent
• Bromazepam: Less potent

• Alprazolam: More likely to cause memory problems, drowsiness, and dependence
• Bromazepam: More likely to cause muscle weakness, fatigue, and dizziness

• Alprazolam: More severe withdrawal symptoms
• Bromazepam: Less severe withdrawal symptoms

• Alprazolam: Widely available in the US and other countries
• Bromazepam: Available in some countries, but not in the US

Drug Interactions

Central Nervous System Depressants

Opioids: Taking alprazolam with opioids, such as hydrocodone or oxycodone, can lead to increased sedation, respiratory depression, and even death. Both opioids and alprazolam have sedative effects on the central nervous system (CNS), and combining them can intensify these effects, leading to significant respiratory suppression.

Benzodiazepines: Combining alprazolam with other benzodiazepines, like diazepam or clonazepam, can enhance sedative effects and increase the risk of dependence. These medications act on the same receptors in the brain, and combining them can potentiate their effects, leading to excessive sedation and drowsiness.

Alcohol: Mixing alprazolam with alcohol can enhance CNS depression, leading to increased sedation, respiratory depression, and an elevated risk of adverse effects. Both alcohol and alprazolam have sedative properties, and combining them can have additive effects on the CNS, potentially impairing coordination, judgment, and cognitive function.

Antidepressants

Selective Serotonin Reuptake Inhibitors (SSRIs): Combining alprazolam with SSRIs, such as fluoxetine or sertraline, can increase the risk of serotonin syndrome. Serotonin syndrome is a potentially life-threatening condition characterized by agitation, confusion, rapid heartbeat, high blood pressure, and hyperthermia. Both medications affect serotonin levels in the brain, and combining them can lead to an excessive accumulation of serotonin.

Tricyclic antidepressants: Taking alprazolam with tricyclic antidepressants, like amitriptyline, can result in increased sedation and anticholinergic effects. Tricyclic antidepressants have sedative properties and can enhance the CNS depressant effects of alprazolam. They can also cause anticholinergic side effects like dry mouth, blurred vision, constipation, and urinary retention.

Anticonvulsants

Carbamazepine: Concurrent use of alprazolam and carbamazepine can reduce the effectiveness of alprazolam. Carbamazepine is an enzyme-inducing anticonvulsant that can increase the metabolism of alprazolam, leading to lower blood levels and potentially decreased therapeutic effects.

Phenytoin: Taking alprazolam with phenytoin can decrease the efficacy of this medicine. Phenytoin is another enzyme-inducing anticonvulsant that can accelerate the metabolism of alprazolam, resulting in lower concentrations of the medication in the body and potentially reduced effectiveness.

Macrolide Antibiotics

Erythromycin and clarithromycin: These macrolide antibiotics can inhibit the metabolism of alprazolam, leading to increased blood levels and a higher risk of toxicity. When alprazolam is taken with erythromycin or clarithromycin, it can lead to excessive sedation, drowsiness, and other adverse effects.

Antifungals

Ketoconazole and itraconazole: Concurrent use of alprazolam with these antifungal medications can inhibit the metabolism of alprazolam, resulting in elevated blood levels. This can increase the risk of alprazolam toxicity and lead to excessive sedation, drowsiness, and other adverse effects.

Stimulants

Amphetamine and cocaine: Combining alprazolam with stimulant drugs like amphetamine or cocaine can have contrasting effects. It is a CNS depressant, while stimulants have stimulating effects on the CNS. Combining these substances can lead to a masking effect, where the sedative effects of alprazolam counteract the stimulating effects of the stimulant drugs. This can potentially lead to an increased risk of dependence and have adverse effects on the cardiovascular system.

Supplements

St. John’s Wort: Taking alprazolam with St. John’s Wort, an herbal supplement used for depression, can reduce the efficacy of alprazolam. St. John’s Wort can induce enzymes in the liver responsible for metabolizing medications, including alprazolam, leading to decreased blood levels and potentially reduced effectiveness.

Grapefruit juice: Consuming grapefruit juice while taking alprazolam can inhibit enzymes in the liver that break down the medication, leading to increased blood levels of this medicine. This can result in higher drug concentrations and an increased risk of toxicity, including excessive sedation and other adverse effects.

Alprazolam Brands in Pakistan

1. Aloram (Global Pharmaceuticals)
2. Alp (Hilton Pharma)
3. Alpamed (Medifine Laboratories)
4. Alpax (Efroze Chemical Industries)
5. Alpram (Akhai Pharmaceuticals)
6. Alpranax (Star Laboratories)
7. Alprazota (Orta Labs)
8. Anpra (Cirin Pharmaceuticals)
9. Anrid (Evron)
10. Anxiorid (Medicraft Pharmaceuticals)
11. Anxnil (Pharmix Laboratories)
12. Anxoten (Bloom Pharmaceuticals)
13. Axal (Amson Vaccines & Pharma)
14. Azolam (Merck Private Ltd)
15. Azolex (Pharmacare Laboratories)
16. Bizolam (Bio Labs)
17. Enzo (Macter International)
18. Hilaxin (Himont Pharmaceuticals)
19. Lampro (Saffron Pharmaceutical Company)
20. Lamzo (Genix Pharma)
21. Lapranx (Bryon Pharmaceuticals)
22. Leazam (Leads Pharma)
23. Lydia (Wilshire Laboratories)
24. Mazolam (Munawar Pharma)
25. Mulis (Pliva Pakistan)
26. Neram (Genix Pharma)
27. Nervin (Werrick Pharmaceuticals)
28. Neuxam (Standpharm Pakistan)
29. Nizam (Universal Pharmaceuticals)
30. Noxalam (Platinum Pharmaceuticals)