GALENICOS BETA-CLEANSE LOTION 10%

Indications

• Prophylaxis of venous thromboembolism following knee replacement surgery
• Prophylaxis of venous thromboembolism following hip replacement surgery
• Treatment of deep vein thrombosis
• Treatment of pulmonary embolism
• Prophylaxis of recurrent deep vein thrombosis
• Prophylaxis of recurrent pulmonary embolism
• Prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation

Dosage

Adults: Initially 10 mg twice daily for 7 days, then maintenance 5 mg twice daily. For the prophylaxis of venous thromboembolism following hip or knee replacement surgery, the recommended dose is 2.5 mg twice daily, to be started 12-24 hours after surgery.

Mechanism of action

Apixaban selectively inhibits factor Xa in both its free and bound forms, independently of antithrombin III. This inhibition prevents the conversion of prothrombin to thrombin, thereby inhibiting thrombus formation.

Pharmacodynamics

The pharmacodynamic effects of apixaban are characterized by its ability to inhibit factor Xa, which plays a crucial role in the coagulation cascade. This leads to decreased thrombin generation, resulting in reduced clot formation. Its anticoagulant effect can be monitored by measuring anti-factor Xa activity.

Pharmacokinetics

Apixaban is rapidly absorbed after oral administration, with peak plasma concentrations reached within 3 to 4 hours. It has a bioavailability of approximately 50% and is primarily metabolized in the liver via cytochrome P450 enzymes, particularly CYP3A4. The elimination half-life ranges from 8 to 15 hours, and the drug is eliminated through both renal and fecal pathways, with about 25% excreted unchanged in urine.

Contra-indications

• Active bleeding
• Severe uncontrolled hypertension
• History of bleeding diathesis
• Significant risk of major bleeding

Adverse effects

• Bleeding complications
• Nausea
• Headache
• Dizziness
• Diarrhea
• Myalgia
• Skin reactions

Interactions

• St. John's Wort (moderate decrease in exposure)
• Antifungals (azoles - potential increased risk of bleeding)
• Calcium channel blockers (unknown effect on exposure)
• Ciclosporin (unknown effect on exposure)
• HIV protease inhibitors boosted with ritonavir or cobicistat (unknown effect on exposure)
• Idelalisib (unknown effect on exposure)
• Lapatinib (unknown effect on exposure)
• Mitotane (unknown decrease in exposure)
• Neratinib (unknown effect on exposure)

Precautions

• Use with caution in the elderly
• Monitor renal function
• Assess risk factors for bleeding before initiation

Pregnancy

Not known to be harmful, but caution is advised.

Breast-feeding

Use only if essential, as small amounts are present in milk.

Storage

Store in the original container with desiccant, discard any remaining capsules 6 weeks after opening.

Formulations

• Tablets: 2.5 mg, 5 mg, and 10 mg
• Modified-release capsules

Indications

• Iodine deficiency
• Goiter
• Hypothyroidism
• Thyroiditis
• Fibrocystic breast disease

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines based on age and weight.

Adults: Refer to the BNF for appropriate dosing guidelines based on condition and clinical judgment.

Mechanism of action

Molecular iodine inhibits the induction and promotion of carcinogenesis in mammary tissues and has shown beneficial effects in fibrocystic breast disease. It temporarily decreases thyroid hormone production through the acute Wolff-Chaikoff effect, followed by a return to normal hormone synthesis due to down regulation of the sodium-iodide symport. This mechanism can lead to a transient hypothyroid state in some individuals with underlying thyroid conditions.

Pharmacodynamics

Iodine is vital for the synthesis of thyroid hormones thyroxine (T4) and triiodothyronine (T3). It affects the metabolism of amine-derived hormones and plays a role in amino acid metabolism. The acute excess of iodide can lead to decreased circulating levels of T4 and T3 in susceptible individuals, while most people can escape this effect and maintain normal thyroid function.

Pharmacokinetics

Iodine is absorbed primarily in the gastrointestinal tract and is distributed throughout the body, particularly in the thyroid gland, where it is concentrated for hormone synthesis. The kidney plays a significant role in the excretion of excess iodine. The half-life of iodine in the body varies and can be influenced by dietary intake and underlying health conditions.

Adverse effects

• Hypothyroidism
• Hyperthyroidism
• Iodine allergy
• Gastrointestinal disturbances

Interactions

• Thyroid hormones
• Antithyroid drugs
• Lithium
• Diuretics

Precautions

• Use with caution in patients with thyroid dysfunction
• Monitor thyroid function periodically during treatment
• Pregnant or breastfeeding women should consult a healthcare provider before use

Pregnancy

Iodine is essential for fetal thyroid hormone synthesis, but excessive iodine intake should be avoided.

Breast-feeding

Iodine is excreted in breast milk; consult a healthcare provider regarding supplementation.

Storage

Store in a cool, dry place away from light.

Formulations

• Iodine solution
• Iodine tincture
• Potassium iodide tablets

Indications

• Topical antiseptic for skin disinfection
• Surgical scrubs and hand sanitizers
• Wound care management
• Pharmaceutical excipient in solid and liquid formulations

Dosage

Children: Refer to specific product guidelines for pediatric dosing recommendations, as doses can vary based on formulation and intended use.

Adults: Refer to specific product guidelines for dosing recommendations, as doses can vary based on the formulation and intended use.

Mechanism of action

Povidone acts by forming a complex with iodine when used as an antiseptic, which releases iodine slowly to exert its antimicrobial effect. The iodine disrupts microbial cell walls and interferes with protein synthesis, leading to cell death. Additionally, as a polymer, povidone can enhance drug solubility and stability by forming a hydrophilic matrix.

Pharmacodynamics

Povidone has a broad spectrum of antimicrobial activity against bacteria, viruses, and fungi. Its antiseptic properties are primarily due to the release of iodine, which is effective in reducing microbial load and preventing infection. The polymer's ability to bind to various substances allows it to be utilized in formulations that require improved stability and solubility.

Pharmacokinetics

Povidone is not absorbed systemically when applied topically, as it remains localized at the site of application. Its pharmacokinetics are largely dependent on the formulation and route of administration, with the polymer being metabolized by hydrolysis and excreted in urine as low-molecular-weight compounds. The release and activity of iodine are influenced by the concentration of povidone and the presence of organic matter.

Adverse effects

• Local irritation
• Allergic reactions
• Skin rashes
• Hypersensitivity reactions

Precautions

• Use with caution in patients with known allergies to iodine or povidone-iodine
• Avoid use in deep puncture wounds or serious burns

Pregnancy

Povidone is generally considered safe for use during pregnancy, but it is advisable to consult a healthcare professional before use.

Breast-feeding

Povidone is considered safe during breastfeeding, but it is recommended to consult a healthcare professional.

Storage

Store at room temperature, away from moisture and heat. Keep the container tightly closed.

Formulations

• Topical solution
• Ointment
• Surgical scrub
• Gauze impregnated with povidone-iodine

Mechanism of action

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III. Apixaban also inhibits prothrominase. These effects prevent the formation of a thrombus.

Pharmacodynamics

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III. Apixaban also inhibits prothrominase. These effects prevent the formation of a thrombus.

Mechanism of action

Molecular iodine is known to inhibit the induction and promotion of N-methyl-n-nitrosourea-induced mammary carcinogenesis, to regress 7,12-dimethylbenz(a)anthracene-induced breast tumors in rats.It has also been shown to have beneficial effects in fibrocystic human breast disease. An acute iodide excess (above the preexisting dietary intake) transiently decreases the production of thyroid hormones in the thyroid gland; this is referred to as the acute Wolff-Chaikoff effect. In normal people, this is followed by a return to normal levels of hormone synthesis, referred to as escape from the acute Wolff-Chaikoff effect, without a significant change in circulating hormone levels. Escape is thought to be the result of down regulation of the sodium-iodide symport (NIS), the iodide transporter in the thyroid gland, resulting in a decrease in the intrathyroidal iodine and the resumption of normal hormone synthesis. An acute or chronic excess of iodide can also decrease circulating T4 and T3 levels and induce a hypothyroid state in some people who have underlying thyroid disorders. These effects are the result of a failure to escape from the acute Wolff-Chaikoff effect. Most people who experience iodine-induced hypothyroidism recover when the excess iodine intake is discontinued.