Penceid - instructions for use, dose, side effects, contraindications

Description:Transparent, colorless to pink or orange, a viscous solution with a mild odor that does not contain mechanical inclusions and crystalline particles.

Pharmacotherapeutic group:NSAIDs

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:

Non-steroidal anti-inflammatory drug for external use. The active substance of the drug, diclofenac, has a pronounced analgesic, anti-inflammatory and antipyretic effect. Diclofenac indiscriminately inhibits cyclooxygenase types 1 and 2 (COX-1 and COX-2), disrupting the metabolism of arachidonic acid and the synthesis of prostaglandins, which are the main link in the development of inflammation.

Pharmacokinetics:

Suction

After applying Penseide in the recommended dose (40 mg of diclofenac sodium / knee) twice daily for 7.5 days, the area under the kinetic curve (AUC₀_-₁₂) and the maximum concentration of diclofenac in plasma (C_mOh) on the first day were 77.27 ng * h / ml and 12.16 ng / ml, respectively. On day 8, the values AUC₀_-₁₂AND FROM_mOh were 204.58 ng * h / ml and 25.24 ng / ml, respectively.

Distribution

Diclofenac binds more than 99% to blood plasma proteins, mainly with albumins.

When applied to the affected joint, the concentration of diclofenac is higher in the synovial fluid than in the plasma.

Metabolism

In the blood plasma and urine, 5 metabolites of diclofenac were determined: 4'-hydroxy-, 5-hydroxy-, 3'-hydroxy-, 4 ', 5-hydroxy- and 3'-hydroxy-4'-methoxy diclofenac. The main metabolite of diclofenac, 4'-hydroxy-diclofenac, whose formation occurs mainly with the participation of the cytochrome P450 isoenzyme CYP2C9, has very low pharmacological activity.

how diclofenac, and the oxidized products of its metabolism, undergo glucuronation or sulfation, followed by excretion with bile.

Acylglucuronation reactions mediated by an isoenzyme UGT2B7, and oxidation reactions mediated by an isoenzyme CYP2C8, may also play a role in the metabolism of diclofenac.

The formation of 5-hydroxy- and 3'-hydroxy-diclofenac occurs with the participation of the cytochrome P450 isoenzyme CYP3A4.

Excretion

Most of the metabolites of diclofenac are excreted by the kidneys or by excretion with bile in the form of sulfated or glucuronated conjugates. Only a small part of diclofenac is excreted unchanged by the kidneys.

Indications:

- Pain in the back with inflammatory and degenerative diseases of the spine (radiculitis, osteoarthritis, lumbago, sciatica);

- pain in the joints (joints of the fingers, knees, etc.) with rheumatoid arthritis, osteoarthritis;

- pain in muscles (due to stretching, overstrain, bruises, injuries);

- inflammation and puffiness of soft tissues and joints due to injuries and rheumatic diseases (tendovaginitis, bursitis, periarticular tissue lesions, wrist syndrome).

Contraindications:

- Hypersensitivity to diclofenac sodium and / or any of the components of the drug;

- pregnancy;

- the period of breastfeeding;

- propensity to occurrence of attacks of a bronchial asthma,acute rhinitis, skin rashes or other allergic reactions with the use of acetylsalicylic acid or other NSAIDs;

- violation of the integrity of the skin in the intended site of application of the drug;

- perioperative period associated with coronary artery bypass surgery;

- age to 18 years (efficacy and safety of the drug are not established).

Carefully:

Preparation Penseyd should be used with caution in hepatic porphyria (exacerbation), erosive-ulcerous lesions of the gastrointestinal tract, severe hepatic dysfunction and / or renal function, disturbance of blood clotting (including hemophilia, elongation of bleeding time, tendency to bleeding, etc. .d.), chronic heart failure, hypertension, significant dehydration with fluid retention and edema, bronchial asthma, in the elderly.

Pregnancy and lactation:

Pregnancy

In the absence of clinical studies on the use of the drug Penseyd data in pregnant women the drug is contraindicated for use during pregnancy (see. Section "Contraindications").

Breast-feeding

It is not established whether the diclofenac in breast milk. In this regard, it is recommended to stop breastfeeding or stop using Penside, comparing the benefits to the mother and the potential risk to the child (see "Contraindications").

Dosing and Administration:

Outwardly.

The recommended dose is 40 mg of diclofenac sodium (2 clicks on the dispenser head) to the affected area 2 times a day. The duration of treatment depends on the indications and the effect observed. Do not use the drug for more than 14 days without a doctor's recommendation.

Preparation for application of the preparation

Before the first use of the vial, it must be brought into operation.

For this:

- Remove the protective cap;

- Take a paper towel and, holding the bottle in an upright position, press the dispenser head 4 times until it stops, directing the jet on the towel. At the same time, the first 2 doses of the drug will be extracted, which should not be used!

- After this, the vial is ready for use.

The above procedure spend only once, before the first use of the drug!

Application of the preparation

- Penseid is applied to the clean, dry surface of the affected area of the body, which does not have any open wounds;

- Remove the protective cap from the vial;

- While holding the bottle at an angle, remove 1 dose of the drug (2 clicks on the dispenser head) on the palm, as shown in Fig. 1;

- Evenly apply the drug to the affected area, trying not to rub the drug into the skin;

- After applying the preparation, wash your hands thoroughly with soap (except when using fingers on the joints);

- Close the bottle with a protective cap.

Special patient groups

Elderly patients (over 65 years of age): the drug should be used with caution in this group of patients with periodic monitoring of kidney function (see section "With caution").

Patients with impaired renal function: the experience of clinical use of Penzaide in patients with severe renal failure is absent. In this regard, care should be taken with the use of Penceid in this group of patients and to monitor the function of the kidneys (see the section "With caution").

Patients with impaired hepatic function: Penseide should be used with caution in patients with severe hepatic impairment (see section "With caution").

Children: efficacy and safety of Penzaide in children under the age of 18 years have not been established (see section "Contraindications").

Side effects:

To denote the frequency of unwanted drug reactions (NLR), the following classification is used: very often (≥ 1/10 cases); often (≥ 1/100, <1/10); infrequently (≥ 1/1000, <1/100); rarely (≥ 1/10000, <1/1000); very rarely (<1/10000) and unknown (the frequency can not be determined from the available data).

Below are the most frequently encountered NLRs with the use of Penseide.

From the skin (reaction in place of application)

Very often: dry skin.

Often: erythema, pruritus, rash, tissue tightening, peeling, bruising.

Infections and invasions

Often: urinary tract infections.

Disorders from the gastrointestinal tract

Often: nausea.

Disturbance of the respiratory system, organs of the chest and mediastinum

Often: nasal congestion.

Other

When using other medicinal forms for external use containing diclofenac, asthma attacks, bronchospastic reactions, photosensitization reactions, bullous dermatitis, generalized skin rash, allergic reactions (urticaria, angioedema), pustular eruptions, dermatitis, swelling of the treated skin area.

Overdose:

Cases of an overdose of Penceyde are unknown.

With accidental ingestion, it is possible to develop systemic NLRs characteristic of NSAIDs, such as: apathy, drowsiness, nausea, vomiting, epigastric pain, gastrointestinal bleeding. There are rare cases of development of arterial hypertension, acute renal failure, respiratory failure and coma.

At casual reception of a preparation inside it is necessary to spend symptomatic treatment: reception from 60 to 100 g of the activated coal. Induction of emesis is not recommended due to the possibility of aspiration and subsequent irritation of the respiratory tract with dimethylsulfoxide contained in the preparation. Hemodialysis and forced diuresis are not effective due to the high degree of binding of diclofenac to blood proteins (more than 99%).

Interaction:

Studies on the study of specific interactions with other drugs have not been conducted.

When used together, the drug Penseid can enhance the effect of drugs that cause photosensitivity.

Joint use of Penseid with other NSAIDs may increase the risk of NLR. In connection with this, the combined use of Penside and oral NSAIDsIt is possible only if the benefit of joint application exceeds the potential risk.

Diclofenac, like other NSAIDs, can affect the activity of prostaglandins in the kidneys and enhance the toxic effects of certain drugs. therefore diclofenac can enhance the nephrotoxicity of cyclosporine when combined. When joint use of the drug Penceid with cyclosporine, it is recommended to monitor the kidney function.

With the joint use of the drug Penceid with methotrexate, the toxic effect of the latter may be enhanced. With the joint use of the drug Penceid with methotrexate, it is recommended to monitor kidney function.

When using oral dosage forms of diclofenac sodium, the following drug interactions were also observed:

Lithium salts

NSAIDs, including diclofenac sodium, increase the concentration of lithium in plasma and reduce the renal clearance of lithium. Similar effects of NSAIDs are due to inhibition of prostaglandin synthesis in the kidneys.

Diuretics

It was shown that NSAIDs, including diclofenac sodium,can reduce the natriuretic effect of furosemide and thiazide diuretics in some patients. A similar effect of NSAIDs is due to the inhibition of prostaglandin synthesis in the kidneys.

Anticoagulants

Joint use of NSAIDs, including diclofenac sodium, and anticoagulants (eg, warfarin) increased the risk of serious gastrointestinal bleeding.

ACE Inhibitors

NSAIDs, including diclofenac sodium, can reduce the antihypertensive effect of ACE inhibitors.

Special instructions:

Penseide should be applied only to intact skin, avoiding contact with open wounds and infected or affected areas of the skin.

Do not allow the drug to enter the mouth. in the eyes and mucous membranes. In case of contact with eyes or mucous membranes, immediately rinse thoroughly with water and consult a doctor.

After applying the drug, do not apply airtight occlusive dressings at the site of application. However, it is recommended to close the place of application of the preparation with a warming bandage or to bandage.

For 30 minutes after applying Penseid, do not take a shower or bath.

If it is necessary to apply other medicinal products for external use or cosmetics, it is necessary to wait until the surface treated with the Penside drug is completely dry.

In case of skin rash or other NLR, including symptoms of hepatotoxicity (nausea, eosinophilia, abdominal pain, weakness, jaundice, diarrhea, influenza-like symptoms, etc.), the drug should be used immediately stop. Avoid direct sunlight or artificial lighting on the surface treated with Penseide.

All NSAIDs, including Penseid. as well as selective and nonselective inhibitors of COX-2, may increase the risk of thrombotic cardiovascular complications, myocardial infarction and stroke. The risk of their development is higher in patients with cardiovascular diseases in the anamnesis.

If, on the background of the use of Penside, patients develop symptoms / signs that indicate a gastrointestinal lesion / disease or ulcerative lesion of the stomach or intestines or bleeding, they should immediately stop using the drug and consult a doctor.For patients with the aforementioned diseases in the history, careful medical observation is recommended in connection with an increased risk of developing gastrointestinal bleeding. This risk increases with the combined use of oral glucocorticosteroids or anticoagulants, smoking, alcohol abuse, prolonged drug therapy or in elderly patients.

It is necessary to control blood pressure before and during the treatment with Penseide in patients with history of arterial hypertension.

Against the background of therapy with NSAIDs, including Penseid, fluid retention and swelling were noted. Therefore, when using Penceide, patients with heart failure should be careful.

As with other NSAIDs, anaphylactoid reactions may develop with the first use of the Penseide drug. In this regard, the use of the drug Penseid is contraindicated in patients who are prone to the occurrence of bouts of bronchial asthma, acute rhinitis, skin rashes or other allergic reactions with the use of acetylsalicylic acid or other NSAIDs (see section "Contraindications").

Given the incidence of anemia in patients taking NSAIDs, the use of Penseid should monitor the concentration of hemoglobin in patients who have symptoms / signs of anemia.

Against the backdrop of the use of Penseide, as with other NSAIDs, serious dermatological reactions such as Stephen-Johnson syndrome, exfoliative dermatitis and toxic epidermal necrolysis, which in some cases may be fatal, can develop. When the first signs of skin rashes or other symptoms of hypersensitivity appear, Penceid immediately stop.

To reduce the risk of developing NLR, Penseide should be used in the lowest effective dose with the shortest course of treatment.

Caution should be exercised in the joint administration of the drug Penceid with potentially hepatotoxic drugs (eg, paracetamol, antiepileptic drugs).

Effect on the ability to drive transp. cf. and fur:

The drug Penceid does not affect the ability to drive vehicles and mechanisms.

Form release / dosage:

Solution for external use, 2%.

Packaging:

For 112 g in a polypropylene / polyethylene / polyester / aluminum bottle with a pump dispenser and a polypropylene cap.

1 bottle with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004098

Date of registration:25.01.2017

Expiration Date:25.01.2022

The owner of the registration certificate:NovaMedika, OOONovaMedika, OOO Russia

Manufacturer: & nbsp

Nuvo Pharmaceuticals Inc. Canada

Representation: & nbspNovaMedika, OOONovaMedika, OOORussia

Information update date: & nbsp28.02.2017

Illustrated instructions

Instructions

Penseid (Penseyd)