SPASMOCARE PLUS TABLETS

Indications

• Abdominal pain
• Dysmenorrhea
• Visceral spasms
• Cervical dilation during labor

Dosage

Children: Refer to the BNF for Children for specific dosing information.

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Drotaverine is an inhibitor of phosphodiesterase 4 (PDE4), an enzyme that degrades cyclic adenosine monophosphate (cAMP). By inhibiting PDE4, drotaverine increases cAMP levels, leading to relaxation of smooth muscles. Additionally, it may exhibit minor allosteric calcium channel blocking effects, acting similarly to voltage-dependent L-type calcium channel blockers.

Pharmacodynamics

Drotaverine is classified as a spasmolytic agent, exerting a relaxing effect on smooth muscles. It effectively relieves visceral spasms and enhances cervical dilation. In vitro studies have shown that drotaverine can induce cytostatic effects on various human tumor cell lines, indicating potential anticancer properties. However, its primary clinical use remains in the management of smooth muscle spasms.

Pharmacokinetics

The pharmacokinetics of drotaverine, including absorption, distribution, metabolism, and excretion, are not detailed in the provided information. General pharmacological knowledge suggests that spasmolytics are typically well-absorbed and distributed widely throughout body tissues, with metabolism primarily occurring in the liver and excretion through urine. For specific pharmacokinetic parameters, further studies or data would be required.

Contra-indications

• Hypersensitivity to drotaverine or any of its excipients
• Severe liver or kidney impairment

Adverse effects

• Nausea
• Vomiting
• Constipation
• Dizziness
• Headache
• Dry mouth
• Allergic reactions

Interactions

• May enhance the effects of other antispasmodics
• Caution when used with other medications that affect smooth muscle tone

Precautions

• Use with caution in patients with hypotension
• Monitor for signs of allergic reactions

Pregnancy

Drotaverine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with a healthcare professional before use.

Breast-feeding

It is not known whether drotaverine is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

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

Formulations

• Tablets
• Injectable solution

Indications

• Mild to moderate pain
• Dysmenorrhea
• Postoperative pain
• Osteoarthritis
• Rheumatoid arthritis

Dosage

Children: For

Adults: The usual adult dose is 500 mg initially, followed by 250 mg every 8 hours as needed. The maximum daily dose should not exceed 2000 mg.

Mechanism of action

Mefenamic acid exerts its therapeutic effect by inhibiting the cyclooxygenase (COX) enzymes, which are responsible for the conversion of arachidonic acid to prostaglandins. By reducing prostaglandin production, mefenamic acid decreases inflammation, pain, and fever. This inhibition primarily occurs through the non-selective blockade of COX-1 and COX-2 isoforms.

Pharmacodynamics

The pharmacodynamics of mefenamic acid involve its analgesic, anti-inflammatory, and antipyretic properties. The drug is effective in reducing pain and inflammation due to its ability to lower prostaglandin levels, which play a key role in the inflammatory response. Mefenamic acid tends to have a rapid onset of action, typically within 1 to 2 hours after administration, and its effects can last for several hours, providing relief from pain.

Pharmacokinetics

Mefenamic acid is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 2 to 4 hours after oral administration. The drug is extensively metabolized in the liver, primarily through glucuronidation, leading to the formation of active and inactive metabolites. It has a relatively long half-life of about 2 to 4 hours, and it is excreted mainly in the urine, both as unchanged drug and as metabolites. The pharmacokinetics can be influenced by factors such as age, liver function, and concurrent medications.

Contra-indications

• Hypersensitivity to mefenamic acid or any of its excipients
• Active or history of peptic ulcer disease
• Severe heart failure
• History of gastrointestinal bleeding or perforation
• Severe hepatic impairment
• Severe renal impairment

Adverse effects

• Gastrointestinal disturbances (nausea, vomiting, diarrhea, constipation)
• Headache
• Dizziness
• Rash
• Elevated liver enzymes
• Renal impairment
• Anaphylactic reactions
• Increased risk of cardiovascular events

Interactions

• Increased exposure when used with regorafenib (severe interaction)

Precautions

• Use with caution in patients with a history of gastrointestinal disorders
• Monitor renal function in patients with compromised renal function
• Caution in patients with cardiovascular diseases
• Caution in the elderly, who may be more susceptible to adverse effects

Pregnancy

Mefenamic acid should be avoided during pregnancy, especially in the third trimester due to risks of fetal cardiovascular effects and potential complications.

Breast-feeding

Use with caution; mefenamic acid is excreted in breast milk, but significant effects on the nursing infant are not expected.

Storage

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

Formulations

• Capsules
• Tablets
• Oral suspension

Mechanism of action

Drotaverine is an inhibitor of phosphodiesterase 4 (PDE4), which is an enzyme responsible for the degradation of cyclic adenosine monophosphate (cAMP). Inhibition of PDE4 leads to elevated levels of cAMP, leading to smooth muscle relaxation. Recent research showed that low levels of cAMP have been associated with brain tumorigenesis, leading to the investigation of PDE4 inhibitors as potential anticancer agents.

Pharmacodynamics

Drotaverine is an e spasmolytic agent with a relaxing effect on smooth muscles. It works to relieve visceral spasms and improve cervical dilation. _In vitro_, drotaverine mediated cytostatic effects on several human tumor cell lines and nonmalignant mouse fibroblasts. Drotaverine may have minor allosteric calcium channel blocking properties: _in vitro_, drotaverine behaves like voltage-dependent L-type calcium channel blockers.