Apra

Apra Uses, Dosage, Side Effects, Food Interaction and all others data.

Apra exhibits analgesic action by peripheral blockage of pain impulse generation. It produces antipyresis by inhibiting the hypothalamic heat-regulating centre. Its weak anti-inflammatory activity is related to inhibition of prostaglandin synthesis in the CNS.

Apra (Acetaminophen) is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centres of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat dissipation.

Trade Name Apra
Generic Paracetamol
Paracetamol Other Names Acenol, Acetaminofén, Acetaminophen, Acétaminophène, APAP, Paracetamol, Paracétamol, Paracetamolum
Type
Formula C8H9NO2
Weight Average: 151.1626
Monoisotopic: 151.063328537
Protein binding

The binding of acetaminophen to plasma proteins is low (ranging from 10% to 25%), when given at therapeutic doses.

Therapeutic Class Non opioid analgesics
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Apra
Apra

Dosage

Apra dosage

Adults and adolescents weighing 50 kg and over: the recommended dosage of Apra IV is 1000 mg every 6 hours or 650 mg every 4 hours, with a maximum single dose of Apra IV of 1000 mg, a minimum dosing interval of 4 hours, and a maximum daily dose of Apra of 4000 mg per day.

Adults and adolescents weighing under 50 kg: the recommended dosage of Apra IV is 15 mg/kg every 6 hours or 12.5 mg/kg every 4 hours, with a maximum single dose of Apra IV of 15 mg/kg, a minimum dosing interval of 4 hours, and a maximum daily dose of Apra of 75 mg/kg per day.

Children >2 to 12 years of age: the recommended dosage of Apra IV is 15 mg/kg every 6 hours or 12.5 mg/kg every 4 hours, with a maximum single dose of Apra IV of 15 mg/kg, a minimum dosing interval of 4 hours, and a maximum daily dose of Apra of 75 mg/kg per day.

Side Effects

As all paracetamol products, adverse drug reactions are rare (>1/10000, <1/1000) or very rare (<1/10000). Frequent adverse reactions at injection site have been reported during clinical trials (pain and burning sensation). Very rare cases of hypersensitivity reactions ranging from simple skin rash or urticaria to anaphylactic shock have been reported and require discontinuation of treatment. Cases of erythema, flushing, pruritus and tachycardia have been reported.

Precaution

Administration of Apra in doses higher than recommended may result in hepatic injury, including the risk of severe hepatotoxicity and death. Do not exceed the maximum recommended daily dose of Apra. Use caution when administering Apra in patients with the following conditions: hepatic impairment or active hepatic disease, alcoholism, chronic malnutrition, severe hypovolemia (e.g., due to dehydration or blood loss), or severe renal impairment (creatinine clearance < 30 ml/min). There were infrequent reports of life-threatening anaphylaxis requiring emergent medical attention. Discontinue Apra IV immediately if symptoms associated with allergy or hypersensitivity occurs. Do not use Apra IV in patients with Apra allergy.

Food Interaction

  • Avoid alcohol. Alcohol may increase the risk of hepatotoxicity.

Volume of Distribution

Volume of distribution is about 0.9L/kg. 10 to 20% of the drug is bound to red blood cells. Acetaminophen appears to be widely distributed throughout most body tissues except in fat.

Half Life

The half-life for adults is 2.5 h after an intravenous dose of 15 mg/kg. After an overdose, the half-life can range from 4 to 8 hours depending on the severity of injury to the liver, as it heavily metabolizes acetaminophen.

Clearance

Adults: 0.27 L/h/kg following a 15 mg/kg intravenous (IV) dose. Children: 0.34 L/h/kg following a 15 mg/kg intravenous (IV dose).

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no studies of intravenous Apra in pregnant women; however, epidemiological data on oral Apra use in pregnant women show no increased risk of major congenital malformations. Animal reproduction studies have not been conducted with IV Apra and it is not known whether Apra IV can cause fetal harm when administered to a pregnant woman. Apra IV should be given to a pregnant woman only if clearly needed. There are no adequate and well-controlled studies with Apra IV during labor and delivery; therefore, it should be used in such settings only after a careful benefit-risk assessment. While studies with Apra IV have not been conducted, Apra is secreted in human milk in small quantities after oral administration.

Contraindication

Apra is contraindicated in patients with known hypersensitivity to its active ingredient or to any of the excipients in the intravenous formulation. Also contraindicated in patients with severe hepatic impairment or severe active liver disease

Special Warning

Pediatric Use: The safety and effectiveness of Apra IV for the treatment of acute pain and fever in pediatric patients ages 2 years and older is supported by evidence from adequate and well-controlled studies of Apra IV in adults.

Geriatric use: No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Patients with Hepatic Impairment: Apra is contraindicated in patients with severe hepatic impairment or severe active liver disease and should be used with caution in patients with hepatic impairment or active liver disease. A reduced total daily dose of Apra may be warranted.

Patients with Renal Impairment: In cases of severe renal impairment (creatinine clearance < 30 ml/min), longer dosing intervals and a reduced total daily dose of Apra may be warranted.

Storage Condition

Store in a cool & dry place & away from children. For single use only. The product should be used within 6 hours after opening. Do not refrigerate or freeze.

Innovators Monograph

You find simplified version here Apra

FAQ

What is Apra?

Apra is a common painkiller used to treat aches and pain. It can also be used to reduce a high temperature. It's available combined with other painkillers and anti-sickness medicines. It's also an ingredient in a wide range of cold and flu remedies.

What are side effects of Apra?

  • Skin rash that may include itchy, red, swollen, blistered or peeling skin.
  • Wheezing.
  • Tightness in the chest or throat.
  • Trouble breathing or talking.
  • Mouth, face, lips, tongue or throat start swelling.

How safe is Apra?

Apra is known to cause liver failure in overdose, but it also causes liver failure in people taking standard doses for pain relief. The risk is only about one in a million, but it is a risk. All these different risks stack up.

What are the types of Apra?

Types of Apra

  • tablets or caplets.
  • capsules.
  • liquid – usually for children.
  • soluble tablets (tablets that dissolve in water to make a drink)
  • suppositories (capsules inserted into the back passage)
  • an injection given into a vein – normally only used in hospital.

What happens if I take Apra without any reason?

Even taking one or two more tablets than recommended can cause serious liver damage and possibly death. Apra overdose is one of the leading causes of liver failure.

Why is Apra bad for our liver?

Apra itself is not toxic, but in large amounts it overwhelms the body's ability to process it safely. This can lead to build up of a toxic metabolite (or break-down product), which binds to liver cells, causing these cells to die.

What are the indications of Apra?

This Apra is used to treat mild to moderate pain (from headaches, menstrual periods, toothaches, backaches, osteoarthritis, or cold/flu aches and pains) and to reduce fever.

What happens if I take Apra on an empty stomach?

Ibuprofen, aspirin and other NSAIDs (non-steroidal anti-inflammatory drugs) can irritate the stomach lining, so it is best to take them with food, or a glass of milk. Apra doesn't irritate the stomach lining so it won't matter if you haven't eaten.

Can Apra help I sleep?

A successful result is one where the pain is reduced by half or more, or where they have no or only mild pain. That result delivers not just on pain, but also improves sleep, depression, quality of life, work, and the ability to get on with life.

How is Apra eliminated from the body?

Apra is readily absorbed from the gastrointestinal tract with peak plasma concentrations occurring about 30 minutes to 2 hours after ingestion. It is metabolised in the liver (90-95%) and excreted in the urine mainly as the glucuronide and sulphate conjugates. Less than 5% is excreted as unchanged Apra.

Is Apra is safe during pregnancy?

Apra is the first choice of painkiller if you're pregnant. Apra been taken by many pregnant women with no harmful effects in the mother or baby.

Is Apra safe during breastfeeding?

Apra is the first choice of painkiller if you're breastfeeding women. It's been taken by many breastfeeding women with no harmful effects in the mother or baby.

How does Apra work?

Apra seems to work by blocking chemical messengers in the brain that tell us we have pain. It also reduces fever by affecting the chemical messengers in an area of the brain that regulates body temperature.

When will I feel better after taking Apra?

Apra takes up to an hour to work. It keeps on working for about 5 hours.

Can I take Apra for a long time?

It's safe to take Apra regularly for many years as long as you don't take more than the recommended dosage.

Will Apra affect my fertility?

There's no firm evidence to suggest that taking Apra will reduce fertility in either men or women.

Will Apra affect my contraception?

Apra doesn't affect any type of contraception including the contraceptive pill or emergency contraception.

Can I drink alcohol with Apra?

Drinking a small amount of alcohol while taking Apra is usually safe. Try to keep to the recommended guidelines of no more than 14 units of alcohol a week. A standard glass of wine (175ml) is 2 units. A pint of lager or beer is usually 2 to 3 units of alcohol.

Is there any food or drink I need to avoid when taking Apra?

You can eat and drink normally while taking Apra. You can safely take Apra (but not ibuprofen) on an empty stomach.


*** Taking medicines without doctor's advice can cause long-term problems.
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