DOLOACT-GEL 2.5%/0.25%W/W GEL

Indications

• Topical pain relief for conditions such as osteoarthritis and neuropathic pain
• Management of postherpetic neuralgia
• Supportive treatment for muscle and joint pain
• Stimulation of digestion and appetite

Dosage

Children: Dosage for pediatric patients should be determined by a healthcare provider, taking into consideration

Adults: Topical formulations generally recommend application to the affected area, with specific dosing instructions provided by the product label. For oral supplements, follow the manufacturer's guidelines or consult a healthcare professional.

Mechanism of action

Capsaicin, the main active component in Capsicum, exerts its effects by binding to the TRPV1 (transient receptor potential vanilloid 1) receptor, which is a cation channel involved in the transmission of pain and heat sensations. This binding leads to the depolarization of sensory neurons, resulting in the release of substance P, a neuropeptide associated with pain signaling. Continuous exposure to capsaicin results in the desensitization of these receptors, leading to decreased pain perception over time.

Pharmacodynamics

The analgesic properties of Capsicum are attributed to its ability to alter the perception of pain. Capsaicin induces a sensation of warmth and pain initially, which is followed by a prolonged analgesic effect due to the depletion of substance P from the nerve endings. Additionally, Capsicum may exhibit anti-inflammatory effects through the modulation of cytokine release and inhibition of inflammatory pathways, contributing to its therapeutic applications in pain management and inflammatory conditions.

Pharmacokinetics

Capsaicin is poorly absorbed when ingested orally, but it can be effectively absorbed through the skin when applied topically. After application, it is metabolized by the liver, and its metabolites are excreted primarily through the kidneys. The onset of action for topical preparations can vary, with effects often observed within hours. The duration of action may last from several hours to days, depending on the formulation and the area of application.

Adverse effects

• Burning sensation at the site of application
• Skin irritation or rash
• Gastrointestinal upset (if ingested)
• Allergic reactions

Precautions

• Avoid contact with eyes and mucous membranes
• Use caution in patients with sensitive skin
• Consult a healthcare professional before use in patients with underlying health conditions

Pregnancy

Capsicum is generally considered unsafe during pregnancy due to potential effects on the fetus. Pregnant women should consult a healthcare provider before use.

Breast-feeding

Capsicum should be used with caution during breastfeeding as it may affect milk production or flavor.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Topical ointments or creams
• Capsules
• Powdered form for oral use

Indications

• Acute pain
• Chronic pain conditions
• Osteoarthritis
• Rheumatoid arthritis
• Ankylosing spondylitis
• Dysmenorrhea
• Postoperative pain

Dosage

Children: For paediatric patients, dosing must be tailored according to weight

Adults: For adults, the dosage of ketoprofen typically ranges from 50 to 100 mg taken every 6 to 8 hours as needed, not exceeding 300 mg per day. However, specific dosing should be referred to the BNF.

Mechanism of action

Ketoprofen exerts its effects by non-selectively inhibiting cyclooxygenase (COX) enzymes, which results in decreased synthesis of prostaglandins. Prostaglandins are mediators of pain and inflammation, and their reduction leads to alleviation of these conditions.

Pharmacodynamics

The analgesic effect of ketoprofen is attributed to its ability to inhibit both COX-1 and COX-2, thereby decreasing the production of prostaglandins that sensitize pain receptors. Its anti-inflammatory action is also linked to its ability to reduce prostaglandin levels, which contribute to the inflammatory response. Additionally, ketoprofen may affect other mediators involved in inflammation and pain pathways.

Pharmacokinetics

Ketoprofen is well absorbed from the gastrointestinal tract, with peak plasma concentrations typically occurring within 1 to 2 hours after oral administration. It has a high protein binding rate (approximately 95%) and a relatively long half-life of around 2 hours. Ketoprofen is metabolized primarily in the liver and excreted via the kidneys. The pharmacokinetics may vary based on the formulation (oral, topical, or parenteral) and patient-specific factors such as age and liver function.

Contra-indications

• Hypersensitivity to ketoprofen or any of its excipients
• Active peptic ulcer disease
• History of gastrointestinal bleeding or perforation related to previous NSAID therapy
• Severe renal impairment
• Severe hepatic impairment
• Pregnancy (third trimester)
• Asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs

Adverse effects

• Gastrointestinal disturbances (nausea, vomiting, diarrhea, constipation)
• Gastrointestinal bleeding
• Renal toxicity (acute kidney injury)
• Hepatic dysfunction
• Cardiovascular events (e.g., myocardial infarction, stroke)
• Skin reactions (rash, pruritus, urticaria)
• Central nervous system effects (headache, dizziness, drowsiness)

Interactions

• Increased risk of gastrointestinal bleeding with other NSAIDs, anticoagulants, or corticosteroids
• May enhance the effects of antihypertensive medications
• Increased plasma concentrations of lithium and methotrexate
• Potentially increased nephrotoxic effects with diuretics and ACE inhibitors

Precautions

• Use with caution in patients with a history of peptic ulcer disease or gastrointestinal bleeding
• Monitor renal function in patients with renal impairment or those taking nephrotoxic agents
• Caution in patients with cardiovascular disease or those at risk of cardiovascular events
• Avoid use in patients with asthma or those with a history of allergic reactions to NSAIDs

Pregnancy

Ketoprofen is contraindicated in the third trimester of pregnancy due to potential risks to the fetus, including cardiovascular and pulmonary complications.

Breast-feeding

Ketoprofen is excreted in breast milk; caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Oral tablets
• Topical gel
• Injection solution

Indications

• Antimicrobial treatment
• Antioxidant therapy
• Flavoring agent in food
• Natural preservative
• Traditional medicine applications

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing.

Adults: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing.

Mechanism of action

The mechanism of action of oleoresin varies depending on its source and the specific compounds it contains. Generally, oleoresins exhibit antimicrobial activity, which may involve the disruption of microbial cell membranes or interference with metabolic processes. Additionally, some components may have anti-inflammatory and antioxidant effects, contributing to their therapeutic potential.

Pharmacodynamics

Oleoresins exhibit a range of pharmacodynamic effects, including antimicrobial, antioxidant, and anti-inflammatory activities. The specific effects will depend on the source of the oleoresin and its chemical composition. These properties are attributed to the various phytochemicals present, such as terpenes, phenolics, and other bioactive compounds, which can modulate biological pathways and influence physiological responses.

Pharmacokinetics

The pharmacokinetics of oleoresin are not well-defined due to the complexity of its composition. Generally, the absorption and metabolism of oleoresins can vary widely based on the individual compounds they contain. Lipophilic components may be absorbed through the gastrointestinal tract and metabolized in the liver, while other components may undergo different metabolic pathways. The elimination half-life is also variable, reflecting the diverse nature of its constituents.

Pregnancy

Safety in pregnancy has not been established, consult healthcare provider.

Breast-feeding

Consult healthcare provider before use during breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight.