orphenadrine/aspirin/caffeine

Action and Spectrum

Actions and Spectrum: 

Actions: 

orphenadrine is a muscle relaxant that blocks the action of acetylcholine, a neurotransmitter involved in muscle contraction. It also has some mild analgesic (pain-relieving) properties.  

aspirin is a NSAID, nonsteroidal anti-inflammatory drug that inhibits the production of prostaglandins, substances involved in pain, inflammation, and fever. 

caffeine is a central nervous system stimulant that blocks adenosine’s action, a neurotransmitter that promotes sleepiness and relaxation. It can also enhance the effects of certain analgesics. 

Spectrum: 

orphenadrine is primarily used to relieve musculoskeletal pain and discomfort associated with muscle spasms. It is commonly prescribed for muscle strains, sprains, and musculoskeletal injuries. 

aspirin has a wide range of uses. It is generally used to relieve pain, reduce inflammation, lower fever, and inhibit platelet aggregation (blood thinning). aspirin is often prescribed for conditions such as headache, fever, mild-to-moderate pain, arthritis, and certain cardiovascular conditions. 

caffeine is primarily used to increase alertness and combat fatigue. Combined with other ingredients, such as orphenadrine and aspirin, it can enhance their analgesic effects and relieve pain, particularly headaches and migraine. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Tachycardia 

Palpitation 

Blurred vision 

Dilated pupils 

Urinary hesitancy or retention 

Dry mouth 

Headache 

Dizziness 

Constipation 

Nausea 

Vomiting 

Drowsiness 

Urticaria (rare) 

Increased intraocular tension 

Weakness 

Other dermatosis (rare) 

Confusion 

Transient episodes of light-headedness 

Aplastic anemia  

Gastrointestinal hemorrhage

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Asthma and respiratory conditions 
• Pregnancy 
• Lactation 
• CNS effects 

Cautions: 

• Cardiovascular disease 
• Kidney impairment 
• Hepatic impairment 
• Pregnancy  
• Lactation 
• CNS effects 

Pregnancy / Lactation

Pregnancy consideration:  

NSAIDs are not meant for pregnant women. 

They may cause defects in the fetus. 

Breastfeeding warnings:  

The safety of the drug during lactation is unknown. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

The pharmacology of orphenadrine/aspirin/caffeine combination medication involves the individual pharmacological actions of its three active ingredients: orphenadrine citrate, aspirin (acetylsalicylic acid), and caffeine. 

Combining these three ingredients in the orphenadrine/aspirin/caffeine combination medication provides a multimodal approach to pain relief. orphenadrine acts as a muscle relaxant, aspirin provides anti-inflammatory and analgesic effects, and caffeine enhances the analgesic properties and can help alleviate headache symptoms. 

Pharmacodynamics: 

orphenadrine causes relaxation of muscles. 

aspirin is responsible for reducing prostaglandins, inflammation, and fever, and it irreversibly inhibits platelet aggregation. 

caffeine stimulates the nervous system and causes vasoconstriction. 

Pharmacokinetics: 

Absorption 

orphenadrine is well absorbed after oral administration. The peak plasma concentration is usually reached within 2 to 3 hours. aspirin gets rapidly absorbed from the GI tract after oral administration. It is absorbed in the upper region of the small intestine. caffeine gets absorbed from the gastrointestinal tract after oral administration. The peak plasma concentration is usually reached within 30 to 120 minutes. 

Distribution 

orphenadrine has a moderate volume of distribution and can cross the blood-brain barrier. It binds extensively to plasma proteins. 

aspirin is widely distributed throughout the body. It also binds to plasma proteins. 

caffeine is widely distributed throughout the body and readily crosses the blood-brain barrier. It is also found in breast milk. caffeine binds to plasma proteins to a moderate extent. 

Metabolism 

orphenadrine undergoes extensive hepatic metabolism, primarily through the cytochrome P450 enzyme system, specifically CYP2B6 and CYP2D6. The major metabolite, norphenadrine, is pharmacologically active. 

aspirin undergoes hydrolysis to salicylic acid in the body. This conversion occurs mainly in the liver through esterases. 

caffeine undergoes hepatic metabolism primarily via cytochrome P450 enzymes, including CYP1A2. The primary metabolites are paraxanthine, theobromine, and theophylline. 

Elimination and Excretion 

orphenadrine and its metabolites are primarily excreted in the urine. The elimination half-life of orphenadrine is approximately 13 to 20 hours. 

Salicylic acid, the primary metabolite of aspirin, is primarily eliminated by renal excretion. The elimination half-life of salicylic acid is variable and can range from 2 to 3 hours at low doses to 15 to 30 hours at higher doses. 

caffeine and its metabolites are mainly excreted in the urine. The elimination half-life of caffeine can vary among individuals but is generally around 3 to 5 hours. 

Adminstartion

Administration: 

orphenadrine/aspirin/caffeine combination medication is typically administered orally in tablets or capsules. The specific dosage and frequency of administration will depend on the formulation and the individual’s condition. It’s essential to follow the instructions provided by your healthcare professional and the medication’s packaging. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: orphenadrine/aspirin/caffeine 

Pronounced as:  or-FEN-a-dreen, AS-pir-in, KAF-feen 

Why do we use orphenadrine/aspirin/caffeine? 

orphenadrine/aspirin/caffeine combination medication is used primarily to relieve musculoskeletal pain and discomfort associated with muscle spasms. Combining these three active ingredients provides a multimodal approach to pain relief with additional benefits.