Paraverin

Paraverin has a combined antispasmodic and analgesic effect.

Indications of the paraverine

It is used to eliminate pain sensations with a weak or moderate degree of intensity. This includes headaches that have a tensile character (acute or chronic).

[1], [2], [3]

Release form

Release of the medicine is made in tablets, in an amount of 10 pieces inside the blister pack. The box contains 1, 3 or 9 of these packages.

[4], [5], [6], [7], [8],

Pharmacodynamics

Paraverin is a complex agent containing 2 active elements: paracetamol, and drotaverin, which is an isoquinoline derivative (it has antispasmodic properties).

Paracetamol.

Paracetamol has an antipyretic and analgesic effect, which is developed by slowing down the processes of binding of PG within the CNS, as well as the PNS (to a lesser extent). Paracetamol blocks the binding or effects of PG (or other components that have a stimulating effect on painful ends).

Drotaverine.

This element has an antispasmodic effect on smooth muscles - by slowing the activity of the enzyme PDE IV. Effectiveness of the effect of drotaverine is dependent on the indices of the enzyme PDE IV inside a variety of tissues (thus the nature of these tissues is not important). This element in high concentrations also causes a slight retarding effect on calcium calmodulin.

[9], [10], [11], [12], [13], [14], [15], [16], [17]

Pharmacokinetics

Paracetamol.

The component is almost completely and quickly absorbed inside the digestive tract. Peak values within the blood plasma are noted after the lapse of 0.5-1 hour.

Half-life is about 1-4 hours. The substance is evenly distributed inside all body fluids. The level of synthesis with a plasma protein is variable.

Paracetamol excretion mainly occurs through the kidneys - in the form of conjugated metabolic products.

Drotaverine.

After ingestion, complete and rapid absorption of the element occurs. Peak plasma parameters are noted after 45-60 minutes. About 95-98% of the substance is synthesized with the protein of the blood plasma (most - with albumin, and in addition with α- and β-globulins).

The time of plasma half-life of drotaverin is 2.4 hours, and the biological half-life is within 8-10 hours. The element accumulates inside the central nervous system, the myocardium with fatty tissues and the lungs with the kidneys, and in addition it penetrates the placenta. Metabolism of drotaverin is carried out inside the liver.

More than 50% of the substance is excreted in the urine, and another 30% - with feces.

Both active elements of the drug do not demonstrate interactions at the level of protein synthesis. In vitro tests, it was noted that paracetamol (a dose corresponding to the drug dosage) does not exert a specific inhibitory effect on the metabolism of drotaverin, while at the same time increasing the duration of its stay unchanged in 2-7 times. Because of this, it is likely that it is able to inhibit the metabolism of drotaverine in in vivo processes.

[18], [19], [20], [21], [22],

Dosing and administration

The medicine is taken orally.

Scheme of application Paraverine:

• adolescents from 12 years, as well as adults: a single dose of 1-2 tablets, which are consumed at intervals of 8 hours *. For a day, a maximum of 6 tablets is allowed **;
• children of the age category 6-12 years: size of a single dose - 0.5 tablets, taken every 10-12 hours *. For a day allowed to consume a maximum of 1-well pill.

* repeated reception of medicines can be carried out only in the presence of the expressed necessity.

** If the therapy lasts more than 3 days, a maximum of 4 tablets are allowed per day.

Therapy without consulting a doctor can last no more than 3 days.

The recommended portion should not be exceeded.

You can not combine the medicine with other medicines, which contain paracetamol.

[28], [29], [30], [31]

Use of the paraverine during pregnancy

Use Paraverin for lactation or pregnancy - contraindicated.

Contraindications

The main contraindications:

• the presence of intolerance with respect to the drug elements;
• disorders of hepatic activity in a serious degree, and in addition a severe stage of liver failure, hyperbilirubinemia of an innate character and constitutional hyperbilirubinemia;
• kidney failure in severe degree and severe forms of disorders of kidney function;
• severe degree of heart failure (low cardiac output syndrome);
• deficiency of the G6PD element in the body;
• expressed degree of anemia, blood diseases, as well as leukopenia;
• alcoholism.

[23], [24], [25], [26]

Side effects of the paraverine

Use of the drug may lead to the appearance of some side effects.

Negative reactions to paracetamol:

• immune manifestations: the development of anaphylaxis, signs of hypersensitivity, including rashes and itching in the epidermis and mucous membranes (often generalized or erythematous rash and urticaria), and in addition Quincke edema, MEE (here Stevens-Johnson syndrome) and TEN;
• disorders in the gastrointestinal tract: epigastric pain or nausea;
• disorders affecting the endocrine system: the development of hypoglycemia, which can lead to hypoglycemic coma;
• manifestations of lymphatic and hematopoietic processes: the appearance of thrombocytopenia, anemia (also hemolytic), agranulocytosis, and in addition, sulf- and methemoglobinemia (dyspnoea, cyanosis and pain in the heart), as well as bruising or bleeding;
• lesions affecting the respiratory system: spasms of the bronchi in people with intolerance to aspirin and other NSAIDs;
• digestive disorders: a disorder of the liver function, an increase in the activity of liver enzymes (usually without the appearance of jaundice).

Negative reactions to drotaverine:

• immune disorders: allergy symptoms, including urticaria, Quincke edema, skin hyperemia, itching and rashes, and in addition chills, fever, a feeling of weakness and an increase in temperature;
• disorders of CAS function: decrease in blood pressure and heart rate;
• manifestations from the NA: dizziness along with headaches, as well as insomnia;
• disorders in the digestive tract: there is constipation or nausea, and besides this vomiting.

[27],

Overdose

Intoxication associated with the action of paracetamol.

The development of liver damage can occur in adults who used 10 + g of paracetamol, and in addition, in children who took 150+ mg / kg of LS.

In people with risk factors (long-term therapy with phenobarbital, primidon, carbamazepine, and besides phenytoin, St. John's wort, rifampicin or other means-inducers of hepatic enzymes, the constant use of ethyl alcohol in large portions, glutathione cachexia (hunger, digestive disorders, HIV -infection, cystic fibrosis, and in addition cachexia)) the use of 5+ g of medicine can cause hepatic damage.

Among the signs of overdose that develop during the first 24 hours: nausea with abdominal pain, and with it pallor and anorexia with vomiting. Hepatic lesions sometimes develop 12-48 hours after poisoning. The disorder of glucose metabolism, as well as the metabolic form of acidosis, can be noted.

If intoxication has a severe form, liver failure can develop into hemorrhages, hypoglycemia, and in addition to coma and encephalopathy. As a result, death may occur.

If kidney failure is acute, against which there is acute tubular necrosis, there is hematuria, severe pain in the lumbar region and proteinuria. This disorder can develop even in people who do not have severe hepatic diseases. In addition, there was an appearance of pancreatitis and cardiac arrhythmia.

Prolonged use of drugs in high dosages can lead to the appearance of violations of the hematopoietic function - neutro-, thrombocyto-, leuko or pancytopenia, and in addition to the aplastic form of anemia and agranulocytosis. Regarding the function of the central nervous system - an overdose leads to an attitude disorder, strong psychomotor agitation and dizziness. The urination system can react with the development of nephrotoxicity (capillary necrosis, colic in the kidney and tubulointerstitial nephritis).

In case of poisoning, the patient will need urgent medical assistance. It should be immediately brought to the hospital, even if early signs of intoxication are not observed. Manifestations may be limited to vomiting with nausea or not reflect the strength of the expression of poisoning and the degree of risk of injury to the body.

It is necessary to consider therapy with activated carbon (in case of taking a large portion of paracetamol in the previous 60 minutes). The indices of the substance inside the plasma should be measured 4+ hours after its use (its earlier values will not be reliable).

Use of N-acetylcysteine is allowed within 24 hours after drug use, but the most complete protective effect will be observed when administered within 8 hours after application of Paraverine. After this time interval, the effectiveness of the antidote is dramatically weakened.

If the patient is not vomiting, oral methionine is suitable as an appropriate alternative (in places where it is difficult to reach the hospital).

Poisoning caused by drotaverine.

Due to intoxication with drotaverine, the following symptoms develop: weakening of the excitation of the heart muscle, AV blockade, and in addition, arrhythmia. If there is severe intoxication, a rhythm of the heartbeat and conduction occurs (this includes a complete blockade in the bundle of the bundle, and in addition, cardiac arrest). These manifestations can cause a fatal outcome.

When poisoning with drotaverine, appropriate symptomatic measures are carried out.

[32], [33], [34], [35],

Interactions with other drugs

Drotaverine.

Combination with levodopa leads to a weakening of the antiparkinsonian effect, possibly strengthening the tremor with rigidity.

Paracetamol.

The rate of absorption of paracetamol can increase when combined with metoclopramide, as well as domperidone; a decrease in the rate of drug absorption is observed when combined with cholestyramine.

Anticoagulant effects of warfarin and other coumarins can be potentiated with continuous and prolonged combined use with paracetamol (with daily intake). This increases the likelihood of bleeding. But if you take the medication periodically, there is no significant effect.

Barbiturates can weaken the antipyretic properties of paracetamol.

Anticonvulsants (including barbiturates with phenytoin and carbamazepine), stimulating the activity of microsomal hepatic enzymes, can increase the toxic properties of paracetamol against the liver - due to the increase in the degree of conversion of the drug into hepatotoxic metabolic products. The combined use of paracetamol and hepatotoxic drugs increases the toxic effect of drugs on the liver.

The combined use of large portions of paracetamol together with isoniazid increases the likelihood of a hepatotoxic syndrome.

Paracetamol weakens the properties of diuretics.

It is forbidden to combine medicine with alcoholic beverages.

[36], [37], [38], [39], [40]

Storage conditions

Paraverin is required to be kept out of the reach of children. The temperature level is a maximum of 25 ° C.

[41], [42], [43], [44], [45], [46]

Shelf life

Paraverin is allowed to be used for 2 years after the release of the drug.

[47], [48]

Application for children

Prescribing drugs to children under the age of 6 is prohibited.

[49], [50], [51]

Analogues

The analogue of the drug is No-spasm.

[52], [53], [54], [55], [56], [57]

Reviews

Paraverin receives good reviews about its drug effectiveness. Of the merits of the drug is also noted for its low cost.