Nervous 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
Fluoxetine N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine Antidepressant
Subclass: Selective Serotonin Reuptake Inhibitor (SSRI)
Depression, OCD, panic disorder Serotonin transporter (SERT) Capsule (10 mg, 20 mg, 40 mg)
Tablet (10 mg, 20 mg)
Oral solution (20 mg/5 mL)
Oral Nausea, insomnia, sexual dysfunction White to off-white crystalline solid Slightly soluble in water pKa = 9.5 Amine, ether, trifluoromethyl
Levetiracetam (2S)-2-(2-oxopyrrolidin-1-yl)butanamide Antiepileptic
Subclass: SV2A protein modulator
Epilepsy, partial onset seizures Synaptic vesicle protein 2A (SV2A) Tablet (250 mg, 500 mg, 750 mg, 1000 mg)
Oral solution (100 mg/mL)
IV solution (100 mg/mL)
Oral, Intravenous Somnolence, dizziness, behavioral changes White to off-white crystalline powder Freely soluble in water pKa = -2 (very weak acid) Amide, pyrrolidone
Memantine 3,5-dimethyladamantan-1-amine Anti-Alzheimer's
Subclass: NMDA receptor antagonist
Moderate to severe Alzheimer's disease N-methyl-D-aspartate (NMDA) receptor Tablet (5 mg, 10 mg)
Oral solution (2 mg/mL)
Oral Dizziness, confusion, headache White to off-white powder Soluble in water pKa = 10.27 Primary amine, adamantane
Propranolol 1-(1-methylethylamino)-3-(1-naphthyloxy)propan-2-ol Beta-blocker
Subclass: Non-selective beta-adrenergic antagonist
Hypertension, angina, migraine prophylaxis β1 and β2 adrenergic receptors Tablet (10 mg, 20 mg, 40 mg, 80 mg)
Extended-release capsule (60 mg, 80 mg, 120 mg, 160 mg)
Oral solution (4 mg/mL, 8 mg/mL)
Oral Bradycardia, fatigue, cold extremities White crystalline powder Slightly soluble in water, soluble in ethanol pKa = 9.45 Secondary amine, ether, alcohol
Haloperidol 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one Antipsychotic
Subclass: Typical (first-generation) antipsychotic
Schizophrenia, acute psychosis, Tourette syndrome Dopamine D2 receptor antagonist Tablet (0.5 mg, 1 mg, 2 mg, 5 mg, 10 mg, 20 mg)
Oral solution (2 mg/mL)
Injection (5 mg/mL)
Oral, Intramuscular, Intravenous Extrapyramidal symptoms, QT prolongation, sedation White to faintly yellowish microcrystalline powder Practically insoluble in water, soluble in alcohol pKa = 8.3 Ketone, alcohol, piperidine, chlorobenzene, fluorobenzene
Gabapentin (2S)-2-(1-(aminomethyl)cyclohexyl)propanoic acid Antiepileptic
Subclass: GABA analogue
Neuropathic pain, epilepsy Voltage-gated calcium channels Capsule (100 mg, 300 mg, 400 mg)
Tablet (600 mg, 800 mg)
Oral solution (250 mg/5 mL)
Oral Dizziness, somnolence, peripheral edema White crystalline powder Freely soluble in water pKa = 3.4 Amine, carboxylic acid
Carbamazepine 5H-dibenzo[b,f]azepine-5-carboxamide Antiepileptic
Subclass: Sodium channel blocker
Epilepsy, trigeminal neuralgia Voltage-gated sodium channels Tablet (100 mg, 200 mg)
Chewable tablet (100 mg)
Suspension (100 mg/5 mL)
Oral Dizziness, drowsiness, nausea White to off-white powder Soluble in water pKa = 13.3 Amide, aromatic
Amitriptyline 3-(dimethylamino)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-carbonitrile Antidepressant
Subclass: Tricyclic antidepressant (TCA)
Depression, neuropathic pain Serotonin and norepinephrine transporters Tablet (10 mg, 25 mg, 50 mg, 75 mg) Oral Dry mouth, sedation, weight gain White to off-white crystalline powder Slightly soluble in water pKa = 9.4 Amine, aromatic
Duloxetine (S)-N-methyl-3-(naphthalen-1-yl)-3-(thiophen-2-yl)propan-1-amine Antidepressant
Subclass: Serotonin-norepinephrine reuptake inhibitor (SNRI)
Depression, anxiety, neuropathic pain Serotonin and norepinephrine transporters Capsule (30 mg, 60 mg) Oral Nausea, dry mouth, fatigue White to off-white powder Slightly soluble in water pKa = 9.3 Amine, ether
Venlafaxine (2-(dimethylamino)-1-(4-methoxyphenyl)ethanol Antidepressant
Subclass: SNRI
Depression, anxiety disorders Serotonin and norepinephrine transporters Capsule (37.5 mg, 75 mg, 150 mg)
Tablet (75 mg, 150 mg)
Oral Nausea, insomnia, sweating White crystalline powder Freely soluble in water pKa = 9.6 Amine, alcohol
Clonazepam 5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one Benzodiazepine
Subclass: Anticonvulsant
Anxiety, panic disorders, epilepsy GABA-A receptor Tablet (0.5 mg, 1 mg, 2 mg)
Oral solution (1 mg/mL)
Oral Drowsiness, fatigue, dizziness White to off-white powder Practically insoluble in water pKa = 2.0 Amine, carbonyl
Olanzapine 2-methyl-4-(4-methyl-1-piperazinyl)thieno[2,3-b]pyridin-3-ol Antipsychotic
Subclass: Atypical antipsychotic
Schizophrenia, bipolar disorder Dopamine and serotonin receptors Tablet (2.5 mg, 5 mg, 10 mg, 15 mg, 20 mg)
Oral solution (10 mg/mL)
Oral Weight gain, sedation, metabolic changes White to yellowish powder Soluble in water pKa = 9.2 Amine, thioether
Sertraline (S)-N, N-dimethyl-3-[(4-fluorophenyl)methyl]phenylpropan-1-amine Antidepressant
Subclass: SSRI
Depression, anxiety disorders Serotonin transporter (SERT) Tablet (50 mg, 100 mg)
Oral concentrate (20 mg/mL)
Oral Diarrhea, insomnia, sexual dysfunction White to off-white powder Freely soluble in water pKa = 9.5 Amine, aromatic
Lisdexamfetamine (S)-N,N-dimethyl-2-phenylpropan-1-amine Stimulant
Subclass: Amphetamine
ADHD, binge eating disorder Dopamine and norepinephrine transporters Capsule (30 mg, 50 mg, 70 mg) Oral Insomnia, decreased appetite, anxiety White to off-white powder Soluble in water pKa = 9.5 Amine, aromatic
Risperidone 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-4H-1-benzopyran-4-one Antipsychotic
Subclass: Atypical antipsychotic
Schizophrenia, bipolar disorder Dopamine and serotonin receptors Tablet (0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg)
Oral solution (1 mg/mL)
Oral Extrapyramidal symptoms, sedation, weight gain White to off-white powder Soluble in water pKa = 7.8 Amine, carbonyl
Methylphenidate 2-[(2R)-2-(4-chlorophenyl)-2-methylamino]propane-1-carboxylic acid Stimulant
Subclass: Dopamine reuptake inhibitor
ADHD, narcolepsy Dopamine transporters Tablet (5 mg, 10 mg, 20 mg)
Extended-release capsule (10 mg, 18 mg, 27 mg)
Oral Insomnia, loss of appetite, headache White crystalline powder Soluble in water pKa = 8.9 Amine, carbonyl
Fentanyl N-phenyl-N-(1-(2-phenylethyl)-4-piperidinyl)propanamide Opioid analgesic
Subclass: Synthetic opioid
Severe pain μ-opioid receptors Patch (12 mcg/hour, 25 mcg/hour, 50 mcg/hour)
Injection (50 mcg/mL)
Transdermal, intravenous Respiratory depression, sedation, nausea White to off-white powder Soluble in organic solvents pKa = 8.6 Aromatic, amine
Bupropion (±)-2-(tert-butylamino)-3′-chloropropiophenone Antidepressant
Subclass: Norepinephrine-dopamine reuptake inhibitor (NDRI)
Depression, smoking cessation Dopamine and norepinephrine transporters Tablet (75 mg, 100 mg, 200 mg) Oral Insomnia, dry mouth, agitation White crystalline powder Freely soluble in water pKa = 8.0 Amine, aromatic
Topiramate 2,3:4,5-bis-O-(1-methyl-ethylidene)-D-fructopyranose Antiepileptic
Subclass: Multiple mechanisms
Epilepsy, migraine prophylaxis Multiple neurotransmitter receptors Tablet (25 mg, 50 mg, 100 mg, 200 mg) Oral Dizziness, fatigue, cognitive effects White to off-white crystalline powder Soluble in water pKa = 9.8 Sugar, sulfate
Tramadol (±)-trans-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol Analgesic
Subclass: Opioid
Moderate to severe pain μ-opioid and norepinephrine/serotonin receptors Tablet (50 mg)
Extended-release tablet (100 mg, 200 mg, 300 mg)
Oral Dizziness, nausea, constipation White crystalline powder Soluble in water pKa = 9.4 Aromatic, 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. Stahl, S. M. (2013). Stahl's Essential Psychopharmacology: Neuroscientific Basis and Practical Applications. 4th ed. Cambridge: Cambridge University Press.