Caffetin

Caffetine is a combination medicine that is most often used to relieve pain, especially headache. This medication includes several active ingredients: paracetamol (an analgesic that reduces pain and fever), caffeine (stimulates the central nervous system, enhances the analgesic effect of paracetamol and reduces drowsiness), and sometimes other ingredients depending on the formulation. Caffeine may also improve mental and physical performance, reducing fatigue and lethargy.

Caffetine is used to treat conditions associated with soreness such as headache, toothache, muscle and joint pain. It can also be effective in relieving menstrual pain. Despite its effectiveness, like any other medical drug, Caffetine has a number of contraindications and side effects. For example, it is not recommended to be taken by people with hypersensitivity to any of the drug's components, in the presence of serious liver and kidney diseases, as well as during pregnancy and lactation without consulting a doctor.

Before you start taking Caffetine or any other medication, it is important to consult your doctor or pharmacist to make sure it is safe and appropriate in your particular case.

Indications Caffetina

1. Headache: This is one of the most common uses for Caffetine, including pain relief for migraines and tension headaches.
2. Toothache: Caffetine may be effective in reducing pain associated with dental problems, including postoperative pain.
3. Menstrual Pain: This medication may help relieve the discomfort and pain associated with the menstrual cycle.
4. Muscle and joint pain: Caffetine is used to relieve muscle and joint pain caused by exercise, injury, or conditions such as arthritis.
5. Acute pain of low to moderate intensity: The drug may be prescribed for short-term relief of acute pain of various origins.
6. Fever: Caffetine may be used to reduce high body temperature and relieve symptoms associated with colds and flu.

Release form

The dosage form and composition may vary depending on the manufacturer and country, but usually Caffetine is available in the following forms:

1. Tablets: Caffetine tablets are the most common form of release. They may contain different dosages of caffeine and ephedrine depending on the specific drug.
2. Capsules: Some manufacturers may produce Caffetine in capsule form. Like tablets, capsules contain a combination of caffeine and ephedrine and are intended to be taken orally.
3. Solution: In some cases, Caffetine may be available as a solution for intravenous or intramuscular injection. This type of release may be used for a faster onset of action of the drug.

Pharmacodynamics

1. Codeine:

   • Opioid agonist: Codeine acts as an agonist of opioid receptors, in particular μ-opioid receptors. This results in decreased sensitivity to pain and reduced activity of nerve signals associated with pain perception.
   • Anti-coughing action: Codeine can inhibit the cough center in the brain, which is why it is used in the treatment of coughs.

2. Caffeine:

   • Central stimulant action: Caffeine is a central nervous system stimulant. It blocks adenosine receptors, which leads to increased neuronal activity and increased production of neurotransmitters such as norepinephrine and dopamine. This increases wakefulness, improves mood and increases physical and mental alertness.

3. Together, these ingredients provide comprehensive relief from pain, cough, fever and muscle spasms.

4. Paracetamol:

   • Analgesic action: Paracetamol has analgesic effect, reducing the synthesis of prostaglandins in the central nervous system.
   • Antipyretic action: Paracetamol reduces body temperature by acting on the thermoregulatory centers in the hypothalamus.

5. Propifenazone:

   • Muscle relaxant effect: Propifenazone has a myorelaxant effect, reducing muscle tension and helping to reduce pain associated with muscle spasms.

Pharmacokinetics

Due to the complex composition of the drug and the lack of specific data regarding its pharmacokinetics in general, as well as the kinetics of each component, information regarding the pharmacokinetics of Caffetin may be limited.

Nevertheless, some common characteristics of the pharmacokinetics of each component can be inferred:

1. Codeine:

   • Absorption: Codeine is rapidly and completely absorbed from the gastrointestinal tract after oral administration.
   • Distribution: It is well distributed in the body and metabolized in the liver to the active metabolite of morphine.
   • Metabolism: Codeine is metabolized in the liver to form morphine by the enzyme cytochrome P450 2D6.
   • Excretion: Codeine and its metabolites are mainly excreted through the kidneys.

2. Caffeine:

   • Absorption: Caffeine is rapidly absorbed from the gastrointestinal tract.
   • Distribution: It is well distributed to all tissues and organs, including the central nervous system.
   • Metabolism: Caffeine is metabolized in the liver to form active metabolites.
   • Excretion: Caffeine and its metabolites are eliminated from the body mainly through the kidneys.

3. Paracetamol:

   • Absorption: Paracetamol is rapidly and completely absorbed from the gastrointestinal tract.
   • Distribution: It is well distributed in the body.
   • Metabolism: Paracetamol is metabolized in the liver to form inactive metabolites, which are excreted by the kidneys.
   • Excretion: It is eliminated from the body mainly through the kidneys as conjugated metabolites.

4. Propifenazone:

   • Absorption: Propifenazone is rapidly absorbed from the gastrointestinal tract.
   • Distribution: It is distributed in the body and has sedative and antihistamine properties.
   • Metabolism: Propifenazone is metabolized in the liver with formation of inactive metabolites.
   • Excretion: It is eliminated from the body mainly through the kidneys.

Dosing and administration

1. Dosage:

   • Caffetine dosage may vary depending on the formulation and the specific drug.
   • Caffetine is usually taken by adults 1-2 tablets (or other dosage form) 2-3 times a day as needed.
   • Children and adolescents are usually prescribed lower doses determined by their doctor according to their age and weight.

2. Method of Application:

   • Caffetine is usually taken orally (orally), with plenty of water.
   • Tablets or capsules should be swallowed whole, without chewing or breaking into pieces.
   • The solution for injection, if available, may be administered intravenously or intramuscularly by medical personnel.

3. Duration of admission:

   • The duration of the course of taking Caffetine is determined by the doctor and may vary depending on the nature of the pain and response to treatment.
   • It is usually recommended to stop taking the drug when your condition improves or as advised by your doctor.

4. Individualized recommendations from a physician:

   • The doctor can recommend individual adjustments to the dosage and regimen of Caffetine, depending on the nature of the pain syndrome and the patient's condition.
   • It is important to strictly follow the doctor's instructions and do not change the dosage or regimen without his permission.

Use Caffetina during pregnancy

The use of such combination therapies during pregnancy requires special attention and risk assessment.

1. Codeine: Codeine, like other opioids, can cross the placental barrier and affect the fetus. Codeine use during pregnancy can increase the risk of problems in the newborn, such as withdrawal syndrome, growth retardation, premature birth and others.
2. Caffeine: Moderate consumption of caffeine during pregnancy is generally not considered dangerous, but avoiding excess is important. Caffeine can cross the placenta, and excessive consumption may be associated with a risk of premature labor and low birth weight.
3. Paracetamol: Paracetamol is generally regarded as a safe analgesic and antipyretic during pregnancy, but you should follow the recommended doses and consult your doctor before starting it.
4. Propifenazone: Propifenazone belongs to the class of antipyretics and analgesics, and its safety during pregnancy also requires further study.

In general, combination medicines containing codeine are often not recommended during pregnancy because of the potential risks to the developing fetus. It is important to discuss all the risks and benefits of such a medicine with your doctor or obstetrician before starting it during pregnancy.

Contraindications

1. Allergic reaction or hypersensitivity: Patients with known hypersensitivity to caffeine, acetaminophen, aspirin, phenylephrine, or other components of Caffetine should not use this drug because of the risk of allergic reactions.
2. Increased bleeding: The use of aspirin in Caffetine may increase the risk of bleeding, so the drug should be used with caution in patients with blood clotting disorders or with concomitant use of anticoagulants.
3. Peptic ulcer disease: Aspirin may irritate the gastric and intestinal mucosa, therefore the use of Caffetine may be contraindicated in patients with peptic ulcer disease.
4. Severe liver or kidney dysfunction: Acetaminophen and aspirin may accumulate in the body in case of liver or kidney dysfunction, which may lead to toxic effects. Therefore, the use of Caffetine may be contraindicated in patients with severe hepatic or renal dysfunction.
5. Cardiovascular disease: The phenylephrine in Caffetine may increase blood pressure, so its use may be contraindicated in patients with serious cardiovascular disease such as hypertension or heart failure.
6. Pregnancy and breastfeeding: The use of aspirin and phenylephrine during pregnancy may be contraindicated due to risk to the fetus. Caffeine and acetaminophen may be safer but also require caution and doctor's advice.
7. Pediatric age: Use of Caffetine in children may be contraindicated due to the high risk of complications, including aspirin-induced Reis disappearance reinfection.

Side effects Caffetina

Some of the most common side effects associated with the components of Caffetine are:

Common side effects:

• Gastrointestinal disorders: Nausea, vomiting, diarrhea or constipation, abdominal pain. These symptoms may occur due to effects on the gastrointestinal tract.
• Dizziness and drowsiness: This can be especially associated with codeine, which acts on the central nervous system.
• Allergic reactions: Urticaria, itching, rash, Quincke's edema. This may be caused by hypersensitivity to any of the drug components.
• Increased heart rate: Caffeine may cause tachycardia or rapid heartbeat.
• High blood pressure: Can also be caused by caffeine, especially in those prone to hypertension.

Less common side effects:

• Psychological dependence: This is especially true for codeine, which can be addictive with long-term use.
• Hepatotoxicity: High doses of paracetamol may cause liver damage.
• Nephrotoxicity: Prolonged use may have adverse effects on the kidneys.
• Hematologic disorders: Changes in blood such as leukopenia, thrombocytopenia.

Very rare and serious side effects:

• Anaphylactic shock: An extremely rare but life-threatening reaction to an allergen.
• Stevens-Johnson syndrome: A rare but serious condition characterized by extensive vesicular detachment of the skin and mucous membranes.
• Toxic epidermal necrolysis: Another rare but life-threatening condition similar to Stevens-Johnson syndrome.

Side effects may vary from mild to serious and depend on the dosage, duration of treatment, and individual sensitivity to the components of the drug.

Overdose

Each of these components has its own toxic effects, and an overdose can lead to serious complications.

1. Codeine: Codeine overdose can cause serious symptoms of respiratory depression, decreased heart rate, drowsiness, apathy, loss of consciousness, and even coma.
2. Caffeine: Caffeine overdose can cause heart arrhythmias, high blood pressure, insomnia, nervousness, anxiety, tremors, and even seizures.
3. Paracetamol: Paracetamol overdose can cause severe liver damage that can be fatal. Symptoms of overdose include nausea, vomiting, abdominal pain, increased levels of liver enzymes in the blood and jaundice.
4. Propifenazone: Propifenazone overdose can cause severe muscle weakness, respiratory muscle paralysis, drowsiness, hypotonia, coma, and even death from respiratory failure.

Interactions with other drugs

1. Drugs that depress the central nervous system: Caffetine may increase the sedative effects of other drugs such as benzodiazepines, sleeping pills, antidepressants and alcohol. This may result in increased drowsiness and slower reaction time.
2. Antiepileptic drugs: Codeine, caffeine and propiphenazone may affect the metabolism of antiepileptic drugs such as carbamazepine and phenytoin, which may lead to changes in their concentration in the blood and, consequently, to an increase or decrease in the effectiveness of treatment.
3. Drugs metabolized through the liver: Paracetamol contained in Caffetine is metabolized in the liver with the participation of cytochrome P450 enzyme. This may affect the metabolism of other medicines metabolized by the same enzymes and lead to an increase or decrease in their effectiveness.
4. Drugs affecting the blood clotting system: Caffeine and paracetamol may increase the effect of anticoagulants such as warfarin, which may increase the risk of bleeding.
5. Blood pressure-enhancing drugs: Caffeine may increase the effects of vasoconstrictors such as adrenaline and norepinephrine, which can lead to an increase in blood pressure and heart rate.
6. Drugs affecting the gastrointestinal tract: Propifenazone may increase the anticholinergic effects of drugs such as anticholinergic antidepressants or antispasmodics, which may result in slower intestinal peristalsis.