Pain relieving suppositories

Pain-relieving suppositories include analgesics – medicinal substances that provide local anesthesia. Medicines of this type are divided into 2 categories by the place of application: rectal and vaginal suppositories.

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Indications anesthetic suppositories

The suppositories are indicated for use as a painkiller in the following cases: postoperative or post-traumatic pain, rheumatic or gynecological pathologies. In addition, for gout, migraine attacks, and other diseases that cause severe pain.

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Release form

Ketonal is a non-hormonal non-narcotic drug, belongs to the group of non-steroidal anti-inflammatory drugs, possessing anti-inflammatory, analgesic and antipyretic properties. It is used to eliminate moderate or severe pain, which can have different origins.

Relief is a medicine that has a complex effect on the mucous membrane of the rectum located near the anus. The drug is in the form of suppositories that help eliminate problems such as anal itching, cracks, hemorrhoids, and eczema. The drug has a hemostatic, analgesic, and wound-healing effect. Among other things, it can be used as a preventive measure against constipation.

Diclofenac has analgesic and anti-inflammatory properties. The drug's dosage form allows it to deliver active components to the affected area faster (without passing through the gastrointestinal tract), thereby significantly reducing the risk of adverse reactions. The drug is often used to treat gynecological pathologies - to get rid of chronic or acute pain in the pelvis, reduce the strength of spasms, and eliminate inflammatory processes.

Flexen suppositories based on ketoprofen have analgesic, anti-inflammatory, antipyretic and antiplatelet properties.

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Pain-relieving suppositories with anesthesin

Anesthesin is a synthetic drug that falls into the category of anesthetic drugs. Suppositories with Anesthesin are used in the complex treatment of hemorrhoids and other diseases of the rectum. The active component of Anesthesin is benzocaine (this is a local anesthetic, among the properties of which is also an antipruritic effect) - it is used to reduce the superficial sensitivity of tissues.

Pain-relieving rectal suppositories

The advantage of analgesic rectal suppositories is that their medicinal components are quickly absorbed into the blood, since they do not need to pass through the liver and gastrointestinal tract. The rectal method of administration also allows you to relieve the digestive system of the drug load, as a result of which suppositories are much less likely to cause nausea and other side effects (in comparison with drugs that are administered orally).

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Pain Relief Suppositories for Children

The most popular painkiller suppositories for children are Movalis, as this drug rarely causes side effects. In addition, small children are often prescribed Ibuprofen suppositories. The drug Cefekon is also effective (it is allowed to be used from the age of 3 months).

Pain-relieving suppositories for radiculitis, lower back pain and joint pain

Rectal suppositories are often used to relieve pain in the lumbar region – they often act as an alternative to analgesic patches. In addition, suppositories are used to eliminate radiculitis – they act as effectively as analgesics. The most common suppositories used to treat joint and lumbar pain are: papaverine, indomethacin, ketanol, voltaren, etc.

NSAID suppositories can act not only as painkillers, they can prevent the development of inflammatory processes, and also have a muscle relaxant effect on the back muscles and damaged areas of the spine. All these properties allow using such suppositories to treat various inflammatory diseases of the musculoskeletal system.

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Pain-relieving suppositories for cystitis

The use of pain-relieving suppositories for cystitis has several advantages:

• The active component enters the bloodstream fairly quickly, bypassing the liver, as a result of which the pain subsides within 30 minutes after the suppository is inserted;
• There is no risk of side effects due to disruption of the digestive system;
• Suppositories, compared to tablet forms of medicine, contain fewer additional elements.

When choosing suppositories to relieve pain in cystitis, you should initially pay attention to drugs that are made from papaverine, which has an analgesic effect, and belladonna extract; Voltaren, Indomethacin, and Sodium Diclofenac are also used.

Pain-relieving suppositories for prostatitis

To relieve and remove pain in acute or chronic prostatitis, suppositories containing promedol or panotopon are used.

In addition, indomethacin is also used - it is an NSAID, which has the following properties: relieves pain, reduces fever, acts as an anti-inflammatory and antiplatelet agent. That is why it is often used in the treatment of prostatitis.

Pain-relieving suppositories for osteochondrosis

Among the pain-relieving suppositories for osteochondrosis, the following drugs are effective:

• Medicines from the Diclofenac category (such as Diclac, Dicloran, Voltaren, as well as Ortofen and Diclobene);
• Ibuprofen category (Gurofen or Dolgit);
• Indomethacin group;
• Ketoprofen drugs (Ketonal and Flexen, as well as Fastum);
• Nimesulides (Nimesin or Nise).

The properties of pain-relieving suppositories are discussed using the example of the drugs Flexen and Diclofenac.

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Pharmacodynamics

Flexen is an NSAID, a derivative of propionic acid. Its properties include antipyretic, analgesic, and anti-inflammatory effects. This drug affects the body by suppressing the activity of COX (this is the main element of the metabolism of eicosatetraenoic acid, which acts as a precursor of prostaglandins (PG), which are the main causative factors in the development of fever and inflammation, as well as pain). The pronounced analgesic effect of ketoprofen appears through 2 mechanisms of action: peripheral (this is an indirect pathway in which PG synthesis is inhibited), and central (in which PG synthesis in the CNS and PNS is slowed down; in addition, the drug affects the bioactivity of other neurotropic substances that participate in the release of pain mediators located in the spinal cord). Along with this, ketoprofen has antibradykinin properties, it normalizes the work of lysosomal membranes, and also significantly slows down the activity of neutrophilic granulocytes in patients suffering from rheumatoid arthritis. Another of its properties is that it prevents platelet aggregation.

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Pharmacokinetics

The maximum saturation in blood plasma is reached 30-40 minutes after the introduction of Diclofenac. No changes in pharmacokinetics are observed after repeated use of the drug. It binds to plasma proteins by more than 99% (mainly with albumins). It passes into the synovial fluid, where it reaches the maximum saturation 2-4 hours later than in plasma. The half-life of the active component from the synovial fluid is 3-6 hours (the saturation of the active component in the synovial fluid after 4-6 hours will exceed the corresponding indicator in plasma, and will remain so for another 12 hours). The metabolism process is carried out due to multiple or single conjugation, as well as hydroxylation with glucuronate. The P450 CYP2C9 system of elements is also involved in metabolism. The decay products have a weaker pharmacological activity compared to diclofenac.

The systemic clearance rate is 350 ml/min, the distribution volume is 550 ml/kg. The half-life from blood plasma is 2 hours. 65% of the drug is excreted through the kidneys as decay products; less than 1% is excreted unchanged, the remainder of the drug is excreted with bile.

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Dosing and administration

Suppositories should be inserted into the anus after defecation. If the patient cannot empty the bowels on his own, he should drink a laxative or do an enema. After defecation, it is necessary to wash the skin in the perineum and the area near the anus with soap and warm water, and then insert the suppository into the anus.

To make the insertion of the drug as convenient as possible, you need to stand on your elbows and knees, or squat down, and then insert the suppository inside using your index finger. The medicine needs to be pushed until the finger is halfway into the anus.

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Use anesthetic suppositories during pregnancy

Most pain-relieving suppositories cannot be used during pregnancy and lactation - such as Relief Ultra, Diclofenac, etc. Also, the use of Ketonal is strictly prohibited in the 3rd trimester, since suppositories can provoke complications during childbirth or postmaturity of the fetus. But in the 1st and 2nd trimesters, in exceptional situations (if the future benefit to the mother outweighs the possible harm to the baby), the use of these suppositories may be allowed.

Contraindications

Contraindications to the use of pain-relieving suppositories include:

• Allergy to various components of the drug;
• Severe diabetes mellitus;
• Tuberculosis;
• High sodium levels in the blood;
• History of rhinitis, urticaria or asthma that developed as a result of using aspirin or other drugs from the NSAID category (Diclofenac, Ibuprofen or Nimesulide, etc.);
• Ulcer of the duodenum or stomach during an exacerbation;
• Intestinal inflammation in the acute stage (such as granulomatous enteritis, ulcerative colitis, etc.);
• Hemophilia or some other problem with blood clotting;
• Severe liver or kidney failure;
• Progressive renal pathologies;
• Decompensation stage of heart failure;
• CABG performed less than 2 months ago;
• Bleeding in any area (cerebral, gastrointestinal, uterine, etc.) or suspicion of it;
• Chronic digestive disorders (belching, diarrhea, bloating, constipation, etc.);
• Children under 15 years old;
• During lactation.

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Side effects anesthetic suppositories

Side effects include allergies in the form of itching and rash at the site of application of the suppository. In addition, pain and irritation in the rectum, bloody discharge with mucus, diarrhea, and tenesmus may occur.

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Interactions with other drugs

Since ketoprofen binds to plasma proteins, when combined with it, it is necessary to reduce the dosage of sulfur-containing drugs, diphenylhydantoin, and anticoagulants.

Combination with diclofenac increases the saturation of digoxin with lithium, quinolone derivatives, indirect anticoagulants, and antidiabetic drugs for oral use in the blood (may cause hyper- or hypoglycemia). In addition, the toxicity of cyclosporine and methotrexate increases, side effects of GCS (gastrointestinal bleeding) may develop. In combination with potassium-sparing diuretics, diclofenac increases the risk of hyperkalemia, and at the same time reduces the effectiveness of this drug. If diclofenac is combined with aspirin, its saturation in plasma (diclofenac) decreases.

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Storage conditions

Pain-relieving suppositories should be kept in a dry place, out of reach of children. The temperature should not exceed 25 ^o C.

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Shelf life

Pain-relieving suppositories are allowed to be used for 2-3 years from the date of manufacture.

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