Muscular System Drugs

Drug Name IUPAC Name Classification (KD Tripathi) Drug Application Receptors Dosage Form Route of Administration Adverse Reactions Appearance Solubility pKa Value Functional Groups
Baclofen 4-amino-3-(4-chlorophenyl)butanoic acid Muscle Relaxant
Subclass: GABA-B receptor agonist		 Treatment of spasticity GABA-B receptors Tablet (10 mg, 20 mg)
Oral solution (5 mg/5 mL)
Intrathecal solution (0.05 mg/mL, 0.5 mg/mL, 2 mg/mL)		 Oral, Intrathecal Drowsiness, dizziness, weakness White to off-white crystalline powder Slightly soluble in water, very slightly soluble in methanol pKa1 = 3.87, pKa2 = 9.62 Carboxylic acid, amine, chlorobenzene
Dantrolene 1-[[5-(4-nitrophenyl)-2-furyl]methylideneamino]imidazolidine-2,4-dione Muscle Relaxant
Subclass: Direct-acting		 Treatment of malignant hyperthermia, chronic spasticity Ryanodine receptors (RyR1) Capsule (25 mg, 50 mg, 100 mg)
Powder for injection (20 mg)		 Oral, Intravenous Hepatotoxicity, drowsiness, dizziness Orange to orange-tan powder Practically insoluble in water, slightly soluble in ethanol pKa = 7.5 Hydantoin, nitro group, furan
Botulinum Toxin Type A 150 kDa neurotoxin produced by Clostridium botulinum Neuromuscular Blocking Agent
Subclass: Presynaptic blocker		 Treatment of muscle spasms, dystonia, cosmetic use SNAP-25 protein Powder for injection (50 units, 100 units, 200 units) Intramuscular injection Muscle weakness, flu-like symptoms White lyophilized powder Soluble in saline solution N/A (protein) Peptide bonds, disulfide bonds
Cyclobenzaprine 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine Muscle Relaxant
Subclass: Centrally acting		 Relief of muscle spasms 5-HT2 receptors Tablet (5 mg, 7.5 mg, 10 mg)
Extended-release capsule (15 mg, 30 mg)		 Oral Drowsiness, dry mouth, dizziness White crystalline powder Freely soluble in water and alcohol pKa = 8.47 Tertiary amine, cycloheptene
Carisoprodol 2-propyl-2-isobutyl-1,3-propanediol Muscle Relaxant
Subclass: Centrally acting		 Management of acute musculoskeletal pain GABA-A receptors Tablet (250 mg, 350 mg) Oral Drowsiness, dizziness White crystalline powder Soluble in alcohol, slightly soluble in water pKa = 9.4 Carboxylic acid, amine
Tizanidine 4-amino-2-(2-azetidinyl)imidazole Muscle Relaxant
Subclass: Alpha-2 adrenergic agonist		 Relief of muscle spasticity Alpha-2 adrenergic receptors Tablet (2 mg, 4 mg, 6 mg)
Capsule (2 mg, 4 mg)		 Oral Drowsiness, dry mouth, hypotension White to off-white crystalline powder Soluble in water pKa = 7.6 Aromatic amine, imidazole
Metaxalone 3-(3,4-dimethoxyphenyl)-4-methyl-1,3-oxazolidin-2-one Muscle Relaxant
Subclass: Centrally acting		 Muscle relaxation, relief of discomfort Not fully understood Tablet (800 mg) Oral Drowsiness, dizziness White crystalline powder Soluble in water pKa = 10.6 Oxazolidinone, methoxy groups
Orphenadrine 1,2-dimethyl-2-(diphenylmethoxy)ethylamine Muscle Relaxant
Subclass: Anticholinergic		 Relief of muscle spasms Muscarinic receptors Tablet (100 mg) Oral Dizziness, dry mouth White crystalline powder Soluble in alcohol pKa = 9.0 Amine, ether
Diazepam 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one Benzodiazepine
Subclass: Anxiolytic		 Management of anxiety, muscle spasms GABA-A receptors Tablet (2 mg, 5 mg, 10 mg) Oral, Intravenous Drowsiness, dizziness White crystalline powder Soluble in alcohol pKa = 3.4 Benzodiazepine, chlorobenzene
Phenobarbital 5-ethyl-5-phenylbarbituric acid Barbiturate
Subclass: Anticonvulsant		 Management of seizures, sedation GABA receptors Tablet (15 mg, 30 mg) Oral Drowsiness, respiratory depression White crystalline powder Soluble in alcohol, slightly soluble in water pKa = 7.3 Barbituric acid
Chlorzoxazone 2-chloro-4-hydroxybenzophenone Muscle Relaxant
Subclass: Centrally acting		 Muscle spasms, discomfort Not fully understood Tablet (500 mg) Oral Drowsiness, gastrointestinal disturbances White crystalline powder Soluble in alcohol pKa = 8.9 Phenol, aromatic
Rizatriptan 3-(2-amino-4-methylphenyl)-4,5-dihydro-1H-imidazole Triptan
Subclass: Migraine medication		 Treatment of acute migraine attacks Serotonin receptors Tablet (5 mg, 10 mg) Oral Dizziness, somnolence White to off-white powder Slightly soluble in water pKa = 8.3 Imidazole, amine
Gabapentin (1-((2-ethoxy-3-phenylpropyl)amino)hexan-1-one) Anticonvulsant
Subclass: Neuropathic pain agent		 Management of neuropathic pain Calcium channels Capsule (100 mg, 300 mg, 400 mg)
Tablet (600 mg, 800 mg)		 Oral Dizziness, fatigue White crystalline powder Soluble in water pKa = 3.8 Amine, carboxylic acid
Pregabalin (S)-3-(aminomethyl)-5-methylhexanoic acid Anticonvulsant
Subclass: Neuropathic pain agent		 Treatment of neuropathic pain, fibromyalgia Calcium channels Capsule (25 mg, 50 mg, 75 mg, 150 mg) Oral Dizziness, somnolence White crystalline powder Soluble in water pKa = 4.0 Carboxylic acid, amine
Sarcosine N-methylglycine Amine
Subclass: Metabolite		 Investigational for treatment of schizophrenia Not well characterized Powder Oral Gastrointestinal upset White crystalline powder Soluble in water pKa = 9.0 Amino acid
Clonidine (2,6-dichlorophenyl)(2-imidazolidinyl)aminomethyl Antihypertensive
Subclass: Alpha-2 adrenergic agonist		 Management of hypertension Alpha-2 adrenergic receptors Tablet (0.1 mg, 0.2 mg, 0.3 mg) Oral Drowsiness, dry mouth White crystalline powder Soluble in water pKa = 7.7 Aromatic amine, imidazole
Cyclobenzaprine 1-(2-methyl-2-phenyl)cyclobenzaprine Muscle relaxant
Subclass: Tricyclic antidepressant derivative		 Relief of muscle spasm associated with acute pain Muscarinic receptors Tablet (5 mg, 10 mg) Oral Drowsiness, dry mouth Off-white crystalline powder Soluble in alcohol, slightly soluble in water pKa = 9.4 Tricyclic compound
Levodopa (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid Antiparkinsonian Agent
Subclass: Dopamine precursor		 Treatment of Parkinson's disease Converted to dopamine, acts on dopamine receptors Tablet (100 mg, 250 mg)
Extended-release tablet (100 mg, 200 mg)
Oral solution (250 mg/25 mL)		 Oral Nausea, dyskinesia, orthostatic hypotension White to off-white crystalline powder Slightly soluble in water, practically insoluble in ethanol pKa1 = 2.32, pKa2 = 9.68, pKa3 = 13.4 Catechol, carboxylic acid, amine

References

  1. Tripathi, K. D. (2013). Essentials of Medical Pharmacology. 7th ed. New Delhi: Jaypee Brothers Medical Publishers.
  2. Brunton, L. L., Hilal-Dandan, R., & Knollmann, B. C. (2017). Goodman & Gilman's: The Pharmacological Basis of Therapeutics. 13th ed. New York: McGraw-Hill Education.
  3. DrugBank Online. (2021). Drug & Drug Target Database. [online] Available at: https://go.drugbank.com/ [Accessed 10 Sep. 2024].
  4. National Center for Biotechnology Information. PubChem Database. [online] Available at: https://pubchem.ncbi.nlm.nih.gov/ [Accessed 10 Sep. 2024].
  5. Rang, H. P., Ritter, J. M., Flower, R. J., & Henderson, G. (2015). Rang & Dale's Pharmacology. 8th ed. Edinburgh: Elsevier Churchill Livingstone.