Pharmacology Flashcards
Acamprosate
Acamprosate;
Mechanism of Action: Modulates glutamatergic neurotransmission by acting on NMDA receptors
Drug Class: Anti-alcohol dependence agent;
Uses: Maintenance of abstinence in alcohol dependence;
Common Side Effects: Diarrhea, nausea, headache, flatulence
Agomelatine
Agomelatine;
Mechanism of Action: Agonist at melatonin receptors (MT1 and MT2), antagonist at 5-HT2C receptors
Drug Class: Antidepressant (melatonergic agonist)
Uses: Treatment of major depressive disorder; Common Side
Effects: Sleep disturbances, headache, nausea.
Alcohol
Alcohol;
Mechanism of Action: CNS depressant; enhances GABA and inhibits NMDA receptor function
Drug Class: CNS depressant
Uses: Sedation, recreational use, or disinhibition (harmful)
Common Side Effects: Drowsiness, nausea, impaired coordination.
Amantadine
Amantadine;
Mechanism of Action: Increases dopamine release, blocks NMDA receptors, weak anticholinergic
Drug Class: Antiviral and anti-Parkinsonian
Uses: Parkinson’s disease, Influenza A prophylaxis
Common Side Effects: Livedo reticularis, confusion, dry mouth.
Amitriptyline
Amitriptyline;
Mechanism of Action: Inhibits serotonin and norepinephrine reuptake (TCA class)
Drug Class: Tricyclic Antidepressant (TCA)
Uses: Depression, neuropathic pain, migraine prophylaxis
Common Side Effects: Drowsiness, dry mouth, weight gain, dizziness.
Amphetamine
Amphetamine;
Mechanism of Action: Increases release of dopamine and norepinephrine from presynaptic neurons and inhibits their reuptake
Drug Class: CNS stimulant
Uses: ADHD, narcolepsy
Common Side Effects: Insomnia, reduced appetite, dry mouth, increased heart rate.
Aripiprazole;
Aripiprazole
Mechanism of Action: Partial agonist at dopamine D2 receptors and serotonin 5-HT1A receptors, antagonist at 5-HT2A receptors
Drug Class: Atypical antipsychotic
Uses: Schizophrenia, bipolar disorder, adjunct in major depressive disorder
Common Side Effects: Weight gain, restlessness, headache, nausea.
Aspirin
Aspirin;
Mechanism of Action: Inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin and thromboxane synthesis
Drug Class: NSAID and antiplatelet agent
Uses: Pain relief, fever, inflammation, cardiovascular event prevention
Common Side Effects: Gastrointestinal upset, bleeding risk, tinnitus (at high doses).
Baclofen
Baclofen;
Mechanism of Action: GABA-B receptor agonist that reduces excitatory neurotransmitter release in the spinal cord
Drug Class: Muscle relaxant
Uses: Spasticity due to multiple sclerosis or spinal cord injury
Common Side Effects: Drowsiness, dizziness, nausea, fatigue.
Benserazide
Benserazide;
Mechanism of Action: Inhibits peripheral decarboxylation of levodopa, increasing its availability in the brain
Drug Class: Dopa decarboxylase inhibitor
Uses: Used with levodopa for Parkinson’s disease
Common Side Effects: Nausea, orthostatic hypotension, dyskinesia (when combined with levodopa)
Buprenorphine
Buprenorphine;
Mechanism of Action: Partial agonist at mu-opioid receptors and antagonist at kappa-opioid receptors
Drug Class: Opioid partial agonist
Uses: Opioid dependence, moderate to severe pain management
Common Side Effects: Nausea, dizziness, constipation, sedation.
Bupropion
Bupropion;
Mechanism of Action: Inhibits norepinephrine and dopamine reuptake (NDRI)
Drug Class: Antidepressant and smoking cessation aid
Uses: Major depressive disorder, smoking cessation
Common Side Effects: Dry mouth, insomnia, weight loss, agitation.
Buspirone
Buspirone; Mechanism of Action: Partial agonist at serotonin 5-HT1A receptors; Drug Class: Anxiolytic; Uses: Generalized anxiety disorder; Common Side Effects: Dizziness, headache, nausea, restlessness.
Caffeine
Caffeine;
Mechanism of Action: Adenosine receptor antagonist, increasing dopamine and norepinephrine release
Drug Class: CNS stimulant
Uses: Fatigue, drowsiness, apnea in premature infants
Common Side Effects: Restlessness, insomnia, tachycardia, gastrointestinal upset.
Cannabis
Cannabis;
Mechanism of Action: Activates CB1 and CB2 cannabinoid receptors, modulating neurotransmitter release
Drug Class: Cannabinoid
Uses: Chronic pain, nausea/vomiting due to chemotherapy, spasticity in multiple sclerosis
Common Side Effects: Drowsiness, dizziness, dry mouth, appetite changes.
Carbamazepine
Carbamazepine;
Mechanism of Action: Blocks voltage-gated sodium channels, reducing neuronal excitability
Drug Class: Anticonvulsant
Uses: Epilepsy, trigeminal neuralgia, bipolar disorder
Common Side Effects: Dizziness, drowsiness, nausea, rash.
Carbidopa
Carbidopa;
Mechanism of Action: Inhibits peripheral decarboxylation of levodopa, increasing its availability in the brain;
Drug Class: Dopa decarboxylase inhibitor
Uses: Used with levodopa for Parkinson’s disease
Common Side Effects: Nausea, dizziness, dyskinesia (when combined with levodopa).
Chlorpromazine
Chlorpromazine;
Mechanism of Action: Dopamine D2 receptor antagonist, also blocks histamine, alpha-adrenergic, and muscarinic receptors
Drug Class: Typical antipsychotic
Uses: Schizophrenia, bipolar mania, severe nausea/vomiting
Common Side Effects: Sedation, weight gain, dry mouth, extrapyramidal symptoms.
Citalopram
Citalopram
Mechanism of Action: Selective serotonin reuptake inhibitor (SSRI)
Drug Class: Antidepressant
Uses: Major depressive disorder, anxiety disorders
Common Side Effects: Nausea, insomnia, dry mouth, sexual dysfunction.
Clonidine
Clonidine;
Mechanism of Action: Alpha-2 adrenergic agonist, reducing sympathetic outflow
Drug Class: Antihypertensive and sedative
Uses: Hypertension, ADHD, opioid withdrawal
Common Side Effects: Drowsiness, dry mouth, dizziness, fatigue
Clozapine
Clozapine;
Mechanism of Action: Dopamine D2 receptor antagonist and serotonin 5-HT2A receptor antagonist
Drug Class: Atypical antipsychotic; Uses: Treatment-resistant schizophrenia
Common Side Effects: Sedation, weight gain, hypersalivation, agranulocytosis (rare but severe)
Cocaine
Cocaine;
Mechanism of Action: Inhibits the reuptake of dopamine, norepinephrine, and serotonin by blocking transporters
Drug Class: Stimulant (illicit)
Uses: Rarely used medically as a local anesthetic
Common Side Effects: Euphoria, tachycardia, hypertension, anxiety, addiction potential.
Delta-9-Tetrahydrocannabinol (THC)
Delta-9-Tetrahydrocannabinol (THC);
Mechanism of Action: Activates CB1 and CB2 cannabinoid receptors
Drug Class: Cannabinoid
Uses: Chronic pain, chemotherapy-induced nausea, appetite stimulation in wasting syndromes
Common Side Effects: Drowsiness, dizziness, dry mouth, impaired memory.
Diazepam
Diazepam;
Mechanism of Action: Enhances the effect of GABA at GABA-A receptors
Drug Class: Benzodiazepine
Uses: Anxiety, seizures, muscle spasms, alcohol withdrawal
Common Side Effects: Drowsiness, dizziness, fatigue, dependence with prolonged use.
Diclofenac
Diclofenac;
Mechanism of Action: Inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis
Drug Class: NSAID
Uses: Pain relief, inflammation, arthritis;
Common Side Effects: Gastrointestinal upset, headache, elevated liver enzymes.
Disulfiram
Disulfiram;
Mechanism of Action: Inhibits aldehyde dehydrogenase, leading to accumulation of acetaldehyde after alcohol consumption
Drug Class: Alcohol deterrent
Uses: Chronic alcohol dependence
Common Side Effects: Nausea, headache, flushing, metallic taste.
Donepezil;
Donepezil;
Mechanism of Action: Reversibly inhibits acetylcholinesterase, increasing acetylcholine levels;
Drug Class: Acetylcholinesterase inhibitor
Uses: Mild to moderate Alzheimer’s disease
Common Side Effects: Nausea, diarrhea, insomnia, bradycardia.
Entacapone;
Entacapone;
Mechanism of Action: Inhibits catechol-O-methyltransferase (COMT), prolonging the effect of levodopa
Drug Class: COMT inhibitor
Uses: Parkinson’s disease (as adjunct to levodopa/carbidopa)
Common Side Effects: Diarrhea, orange discoloration of urine, dyskinesia.
Ecstasy (MDMA)
Ecstasy (MDMA);
Mechanism of Action: Increases release and inhibits reuptake of serotonin, dopamine, and norepinephrine
Drug Class: Stimulant and empathogen (illicit)
Uses: Experimental in PTSD therapy
Common Side Effects: Hyperthermia, dehydration, anxiety, tachycardia.
Escitalopram
Escitalopram;
Mechanism of Action: Selective serotonin reuptake inhibitor (SSRI);
Drug Class: Antidepressant
Uses: Major depressive disorder, anxiety disorders
Common Side Effects: Nausea, insomnia, sexual dysfunction, dizziness.
Ethosuximide
Ethosuximide;
Mechanism of Action: Inhibits T-type calcium channels in thalamic neurons
Drug Class: Anticonvulsant
Uses: Absence seizures
Common Side Effects: Nausea, dizziness, lethargy, rash.
Flumazenil;
Flumazenil;
Mechanism of Action: Competitive antagonist at benzodiazepine binding sites on the GABA-A receptor
Drug Class: Benzodiazepine antagonist
Uses: Reversal of benzodiazepine sedation or overdose
Common Side Effects: Nausea, vomiting, dizziness, seizures (rare).
Fluoxetine
Fluoxetine;
Mechanism of Action: Selective serotonin reuptake inhibitor (SSRI);
Drug Class: Antidepressant
Uses: Major depressive disorder, obsessive-compulsive disorder (OCD), bulimia nervosa
Common Side Effects: Nausea, insomnia, sexual dysfunction, agitation.
Flupenthixol
Flupenthixol; Mechanism of Action: Dopamine D2 receptor antagonist; Drug Class: Typical antipsychotic; Uses: Schizophrenia, psychosis; Common Side Effects: Sedation, dry mouth, extrapyramidal symptoms.
Fluphenazine
Fluphenazine;
Mechanism of Action: Dopamine D2 receptor antagonist
Drug Class: Typical antipsychotic; Uses: Schizophrenia, psychosis
Common Side Effects: Sedation, weight gain, extrapyramidal symptoms.
Fremanezumab
Fremanezumab;
Mechanism of Action: Monoclonal antibody targeting calcitonin gene-related peptide (CGRP)
Drug Class: Anti-CGRP monoclonal antibody
Uses: Migraine prevention
Common Side Effects: Injection site reactions, fatigue, constipation.
Gabapentin
Gabapentin;
Mechanism of Action: Binds to voltage-gated calcium channels, reducing excitatory neurotransmitter release
Drug Class: Anticonvulsant and analgesic
Uses: Neuropathic pain, partial seizures
Common Side Effects: Drowsiness, dizziness, weight gain
Galantamine
Galantamine;
Mechanism of Action: Reversible acetylcholinesterase inhibitor, enhancing cholinergic function
Drug Class: Acetylcholinesterase inhibitor
Uses: Mild to moderate Alzheimer’s disease
Common Side Effects: Nausea, vomiting, diarrhea, dizziness.
Haloperidol;
Haloperidol;
Mechanism of Action: Dopamine D2 receptor antagonist
Drug Class: Typical antipsychotic
Uses: Schizophrenia, psychosis, agitation, Tourette syndrome
Common Side Effects: Extrapyramidal symptoms, sedation, weight gain.
Heroin
Heroin;
Mechanism of Action: Converts to morphine in the body and activates mu-opioid receptors
Drug Class: Opioid (illicit); Uses: None (illicit drug)
Common Side Effects: Euphoria, respiratory depression, constipation, addiction potential.
Ibuprofen
Ibuprofen;
Mechanism of Action: Inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis
Drug Class: NSAID
Uses: Pain relief, fever, inflammation
Common Side Effects: Gastrointestinal upset, headache, dizziness.
Imipramine
Imipramine;
Mechanism of Action: Inhibits serotonin and norepinephrine reuptake (TCA class)
Drug Class: Tricyclic Antidepressant (TCA)
Uses: Depression, nocturnal enuresis
Common Side Effects: Dry mouth, drowsiness, weight gain, orthostatic hypotension.
Interferon beta-1a
Interferon beta-1a;
Mechanism of Action: Modulates immune response by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines
Drug Class: Immunomodulator
Uses: Relapsing-remitting multiple sclerosis
Common Side Effects: Flu-like symptoms, injection site reactions, fatigue.
Interferon beta-1b;
Interferon beta-1b;
Mechanism of Action: Similar to interferon beta-1a, modulates immune response and reduces inflammation in the CNS
Drug Class: Immunomodulator
Uses: Relapsing-remitting multiple sclerosis
Common Side Effects: Flu-like symptoms, injection site reactions, headache.
Isoflurane
Isoflurane;
Mechanism of Action: Increases GABAergic activity and reduces excitatory neurotransmission
Drug Class: Inhalational anesthetic
Uses: Induction and maintenance of general anesthesia
Common Side Effects: Hypotension, nausea, shivering, malignant hyperthermia (rare).
Ketamine
Ketamine;
Mechanism of Action: NMDA receptor antagonist, reduces excitatory neurotransmission
Drug Class: Dissociative anesthetic
Uses: Anesthesia, treatment-resistant depression, acute pain management
Common Side Effects: Dissociation, hallucinations, dizziness, increased blood pressure.
Lamotrigine
Lamotrigine;
Mechanism of Action: Inhibits voltage-gated sodium channels, stabilizing neuronal membranes
Drug Class: Anticonvulsant
Uses: Epilepsy, bipolar disorder
Common Side Effects: Rash (including Stevens-Johnson syndrome), dizziness, nausea.
Levodopa
Levodopa;
Mechanism of Action: Precursor to dopamine, converted to dopamine in the brain
Drug Class: Dopaminergic agent
Uses: Parkinson’s disease
Common Side Effects: Nausea, dyskinesia, orthostatic hypotension.
Levetiracetam
Levetiracetam;
Mechanism of Action: Modulates synaptic vesicle protein 2A (SV2A), reducing neurotransmitter release
Drug Class: Anticonvulsant
Uses: Epilepsy (partial and generalized seizures)
Common Side Effects: Fatigue, dizziness, irritability.
Lidocaine
Lidocaine;
Mechanism of Action: Blocks voltage-gated sodium channels, preventing nerve impulse conduction
Drug Class: Local anesthetic and antiarrhythmic
Uses: Local anesthesia, ventricular arrhythmias
Common Side Effects: Numbness, dizziness, low blood pressure.
Lithium
Lithium;
Mechanism of Action: Modulates neurotransmission through effects on sodium transport and second messenger systems (e.g., IP3 and cAMP)
Enhances neurogenesis and reduces suicidality; by increasing GABA + serotonin, however, requires careful monitoring due to kidney toxicity
Drug Class: Mood stabilizer
Uses: Bipolar disorder, acute mania
Common Side Effects: Tremor, weight gain, polyuria, hypothyroidism.
N.b. Polyuria and NDI major risk factors for HYPERNATRAEMIA (lithium can cause hypernatraemia)
Lorazepam
Lorazepam;
Mechanism of Action: Enhances GABA activity at GABA-A receptors;
Drug Class: Benzodiazepine
Uses: Anxiety, status epilepticus, alcohol withdrawal
Common Side Effects: Drowsiness, dizziness, dependence, respiratory depression (in high doses)
Memantine
Memantine;
Mechanism of Action: NMDA receptor antagonist, modulating glutamate activity
Drug Class: Cognitive enhancer
Uses: Moderate to severe Alzheimer’s disease
Common Side Effects: Dizziness, headache, confusion, constipation.
Methadone
Methadone;
Mechanism of Action: Long-acting mu-opioid receptor agonist
Drug Class: Opioid
Uses: Opioid dependence, chronic pain
Common Side Effects: Constipation, drowsiness, sweating, risk of respiratory depression
Methysergide
Methysergide;
Mechanism of Action: Serotonin receptor antagonist, particularly at 5-HT2 receptors
Drug Class: Serotonin receptor antagonist
Uses: Migraine prophylaxis (rarely used now)
Common Side Effects: Nausea, abdominal pain, fibrosis (rare but severe)
Mirtazapine
Mirtazapine;
Mechanism of Action: Antagonist at presynaptic alpha-2 adrenergic receptors, increasing norepinephrine and serotonin release
Drug Class: Antidepressant
Uses: Major depressive disorder, insomnia
Common Side Effects: Weight gain, sedation, dry mouth, dizziness
Moclobemide
Moclobemide;
Mechanism of Action: Reversible inhibitor of monoamine oxidase A (RIMA), increasing serotonin, norepinephrine, and dopamine levels
Drug Class: MAOI (monoamine oxidase inhibitor)
Uses: Depression
Common Side Effects: Nausea, dizziness, insomnia, agitation
Morphine
Morphine;
Mechanism of Action: Activates mu-opioid receptors, reducing pain perception
Drug Class: Opioid analgesic
Uses: Severe pain, palliative care
Common Side Effects: Constipation, nausea, drowsiness, respiratory depression.
Naloxone
Naloxone;
Mechanism of Action: Competitive antagonist at opioid receptors, reversing opioid effects
Drug Class: Opioid antagonist
Uses: Opioid overdose reversal
Common Side Effects: Withdrawal symptoms (e.g., agitation, nausea, sweating).
Naltrexone
Naltrexone;
Mechanism of Action: Competitive antagonist at opioid receptors, blocks euphoric effects of opioids and alcohol
Drug Class: Opioid antagonist
Uses: Alcohol and opioid dependence
Common Side Effects: Nausea, headache, dizziness, fatigue.
Is naltrexone the same as naloxone?NO!!!. Naltrexone is used to help people cut down on drinking or to stop drinking alcohol altogether, or to maintain abstinence from opioid drugs. Naloxone is used as an emergency method to reverse an opioid overdose.
Natalizumab
Natalizumab;
Mechanism of Action: Monoclonal antibody that inhibits leukocyte adhesion by binding to integrin alpha-4, reducing CNS inflammation
Drug Class: Immunomodulator; Uses: Relapsing-remitting multiple sclerosis, Crohn’s disease
Common Side Effects: Headache, fatigue, increased risk of progressive multifocal leukoencephalopathy (PML).
Nicotine
Nicotine;
Mechanism of Action: Agonist at nicotinic acetylcholine receptors, enhancing dopamine release
Drug Class: Stimulant and dependency-forming substance
Uses: Smoking cessation (in controlled forms)
Common Side Effects: Increased heart rate, nausea, dizziness, addiction
Nitrous Oxide
Nitrous Oxide;
Mechanism of Action: NMDA receptor antagonist, increases GABAergic activity
Drug Class: Inhalational anesthetic
Uses: Procedural sedation, pain relief during childbirth
Common Side Effects: Dizziness, nausea, hypoxia (if misused)
Olanzapine
Olanzapine;
Mechanism of Action: Antagonist at dopamine D2 and serotonin 5-HT2A receptors
Drug Class: Atypical antipsychotic
Uses: Schizophrenia, bipolar disorder, agitation
Common Side Effects: Weight gain, sedation, hyperglycemia.
Ondansetron
Ondansetron;
Mechanism of Action: Selective serotonin 5-HT3 receptor antagonist;
Drug Class: Antiemetic
Uses: Prevention of nausea and vomiting (e.g., post-surgery, chemotherapy);
Common Side Effects: Headache, constipation, dizziness.
Paracetamol (Acetaminophen);
Paracetamol (Acetaminophen);
Mechanism of Action: Inhibits prostaglandin synthesis in the CNS, with weak COX-2 inhibition peripherally
Drug Class: Analgesic and antipyretic
Uses: Pain relief, fever
Common Side Effects: Rare at therapeutic doses, hepatotoxicity (in overdose).
Perampanel
Perampanel;
Mechanism of Action: Selective non-competitive AMPA receptor antagonist, reducing excitatory neurotransmission
Drug Class: Anticonvulsant
Uses: Epilepsy (partial and generalized seizures)
Common Side Effects: Dizziness, drowsiness, aggression.
Phenelzine
Phenelzine;
Mechanism of Action: Irreversible inhibitor of monoamine oxidase A and B, increasing serotonin, norepinephrine, and dopamine levels
Drug Class: Monoamine oxidase inhibitor (MAOI)
Uses: Depression (refractory cases)
Common Side Effects: Hypotension, weight gain, insomnia, dietary interactions (tyramine).
Phenobarbital
Phenobarbital;
Mechanism of Action: Enhances GABA activity by prolonging the opening of GABA-A receptor chloride channels
Drug Class: Barbiturate
Uses: Epilepsy (tonic-clonic and partial seizures), sedation
Common Side Effects: Drowsiness, dependence, respiratory depression.
Phenytoin
Phenytoin;
Mechanism of Action: Blocks voltage-gated sodium channels, stabilizing neuronal membranes
Drug Class: Anticonvulsant; Uses: Epilepsy (tonic-clonic and partial seizures), status epilepticus
Common Side Effects: Gingival hyperplasia, nystagmus, dizziness, rash.
Pramipexole
Pramipexole;
Mechanism of Action: Dopamine receptor agonist, primarily targeting D2 and D3 receptors
Drug Class: Dopaminergic agent
Uses: Parkinson’s disease, restless legs syndrome
Common Side Effects: Nausea, dizziness, hallucinations, impulse control disorders.
Pregabalin
Pregabalin;
Mechanism of Action: Binds to voltage-gated calcium channels, reducing neurotransmitter release
Drug Class: Anticonvulsant and analgesic
Uses: Neuropathic pain, epilepsy, generalized anxiety disorder
Common Side Effects: Drowsiness, dizziness, weight gain, dry mouth.
Propofol
Propofol;
Mechanism of Action: Enhances GABAergic activity at GABA-A receptors
Drug Class: Intravenous anesthetic
Uses: Induction and maintenance of general anesthesia, sedation
Common Side Effects: Hypotension, bradycardia, pain at injection site.
Rasagiline
Rasagiline;
Mechanism of action; reversible inhibitor of monoamine oxidase B (MAO-B), increasing dopamine levels in the brain
Drug Class: MAO-B inhibitor
Uses: Parkinson’s disease
Common Side Effects: Nausea, headache, orthostatic hypotension
Reboxetine
Reboxetine;
Mechanism of Action: Selective norepinephrine reuptake inhibitor (NRI)
Drug Class: Antidepressant
Uses: Major depressive disorder
Common Side Effects: Dry mouth, insomnia, dizziness, constipation
Risperidone
Risperidone;
Mechanism of Action: Antagonist at dopamine D2 and serotonin 5-HT2A receptors
Drug Class: Atypical antipsychotic
Uses: Schizophrenia, bipolar disorder, irritability in autism
Common Side Effects: Weight gain, sedation, hyperprolactinemia.
Rivastigmine
Rivastigmine;
Mechanism of Action: Reversible inhibitor of acetylcholinesterase and butyrylcholinesterase, increasing acetylcholine levels
Drug Class: Acetylcholinesterase inhibitor
Uses: Mild to moderate Alzheimer’s disease, Parkinson’s dementia
Common Side Effects: Nausea, vomiting, diarrhea, dizziness.
Ropinirole
Ropinirole;
Mechanism of Action: Dopamine receptor agonist, primarily targeting D2 and D3 receptors
Drug Class: Dopaminergic agent
Uses: Parkinson’s disease, restless legs syndrome
Common Side Effects: Nausea, dizziness, hallucinations, impulse control disorders.
Rotigotine
Rotigotine;
Mechanism of Action: Dopamine receptor agonist delivered via a transdermal patch
Drug Class: Dopaminergic agent
Uses: Parkinson’s disease, restless legs syndrome
Common Side Effects: Skin irritation, nausea, dizziness, hallucinations.
Safinamide
Safinamide;
Mechanism of Action: Reversible inhibitor of monoamine oxidase B (MAO-B), increasing dopamine levels in the brain
Drug Class: MAO-B inhibitor
Uses: Parkinson’s disease (adjunct therapy)
Common Side Effects: Nausea, insomnia, headache.
Selegiline
Selegiline;
Mechanism of Action: Irreversible inhibitor of monoamine oxidase B (MAO-B), increasing dopamine availability
Drug Class: MAO-B inhibitor
Uses: Parkinson’s disease, depression (rarely used for this now)
Common Side Effects: Nausea, headache, insomnia, orthostatic hypotension.
Sertraline
Sertraline;
Mechanism of Action: Selective serotonin reuptake inhibitor (SSRI); Drug Class: Antidepressant
Uses: Major depressive disorder, anxiety disorders, OCD, PTSD
Common Side Effects: Nausea, insomnia, sexual dysfunction, dry mouth.
Sodium Valproate
Sodium Valproate;
Mechanism of Action: Increases GABA levels and blocks voltage-gated sodium channels
Drug Class: Anticonvulsant and mood stabilizer
Uses: Epilepsy, bipolar disorder, migraine prophylaxis
Common Side Effects: Weight gain, nausea, hair loss, teratogenicity
Sumatriptan
Sumatriptan;
Mechanism of Action: Agonist at serotonin 5-HT1B and 5-HT1D receptors, causing vasoconstriction and reducing inflammation
Drug Class: Triptan (anti-migraine agent)
Uses: Acute migraine, cluster headaches
Common Side Effects: Flushing, dizziness, chest discomfort.
Tetrabenazine
Tetrabenazine;
Mechanism of Action: Inhibits vesicular monoamine transporter 2 (VMAT2), reducing dopamine release
Drug Class: Dopamine depleting agent
Uses: Huntington’s disease, tardive dyskinesia
Common Side Effects: Sedation, depression, parkinsonism
Tiagabine
Tiagabine;
Mechanism of Action: Inhibits GABA reuptake, increasing GABA availability in the synaptic cleft
Drug Class: Anticonvulsant
Uses: Epilepsy (partial seizures)
Common Side Effects: Dizziness, fatigue, nausea, confusion.
Tolcapone
Tolcapone;
Mechanism of Action: Inhibits catechol-O-methyltransferase (COMT), prolonging levodopa’s effects
Drug Class: COMT inhibitor
Uses: Parkinson’s disease (adjunct therapy)
Common Side Effects: Diarrhea, hepatotoxicity, orange discoloration of urine.
Topiramate
Topiramate;
Mechanism of Action: Blocks voltage-gated sodium channels, enhances GABA activity, and antagonizes AMPA/kainate glutamate receptors
Drug Class: Anticonvulsant
Uses: Epilepsy, migraine prophylaxis
Common Side Effects: Drowsiness, weight loss, cognitive slowing, paresthesia.
Tramadol;
Tramadol;
Mechanism of Action: Weak mu-opioid receptor agonist and serotonin-norepinephrine reuptake inhibitor (SNRI)
Drug Class: Opioid analgesic
Uses: Moderate to severe pain
Common Side Effects: Nausea, dizziness, constipation, dependence
Trazodone
Trazodone;
Mechanism of Action: Antagonist at serotonin 5-HT2A receptors and weak serotonin reuptake inhibitor
Drug Class: Antidepressant
Uses: Depression, insomnia
Common Side Effects: Sedation, dizziness, dry mouth, priapism (rare
Venlafaxine
Venlafaxine;
Mechanism of Action: Serotonin-norepinephrine reuptake inhibitor (SNRI)
Drug Class: Antidepressant
Uses: Major depressive disorder, generalized anxiety disorder, panic disorder
Common Side Effects: Nausea, dizziness, hypertension, insomnia.
Vigabatrin
Vigabatrin;
Mechanism of Action: Irreversibly inhibits GABA transaminase, increasing GABA levels
Drug Class: Anticonvulsant
Uses: Epilepsy, infantile spasms
Common Side Effects: Visual field loss (serious), fatigue, dizziness.
Zopiclone
Zopiclone;
Mechanism of Action: Modulates GABA-A receptors, enhancing GABA activity
Drug Class: Hypnotic; Uses: Insomnia (short-term use)
Common Side Effects: Drowsiness, dry mouth, metallic taste.
Zolpidem
Zolpidem;
Mechanism of Action: Modulates GABA-A receptors, enhancing GABA activity
Drug Class: Hypnotic
Uses: Insomnia (short-term use)
Common Side Effects: Drowsiness, dizziness, headache, confusion
define the following;
- ligand
- cognate ligand
- agonist
- antagonist
ligand= any chemical which combines with a receptor
cognate ligand= endogenous ligand for a receptor
agonist= a ligand that binds to a receptor and alters it’s receptor state, resulting in a biological response n.b. Agonists are drugs with both affinity (they bind to the target receptor) and intrinsic efficacy (they change receptor activity to produce a response)
antagonist= a drug that reduces the action of another ligand/ drug (generally an agonist reducer) e.g. Antagonists have affinity but zero intrinsic efficacy; therefore they bind to the target receptor but do not produce a response.
define intrinsic efficacy
intrinsic efficacy =the capacity of a drug to activate or inactivate a receptor i.e. degree to which an agonist evokes a cellular response
Receptors are allosteric proteins (they change from one folding conformation to a different one when another binds to it); here I’ve listed the fastest to slowest responding receptors in order; explain them + give some examples of each
- ligand gated ion channel (milliseconds)
- GPCR (seconds)
- receptor tyrosine kinase/enzymes (minutes-hours)
- nuclear receptor (hours)
Fastest → Ligand-Gated Ion Channels (Milliseconds) → Direct binding of a ligand opens ion channel + allows rapid ion flow= fast synaptic transmission (e.g., nicotinic AChR, GABA-A receptor, NMDA/AMPA Glutamate receptors).
Intermediate → GPCRs (Seconds) → G-protein signaling (e.g., β-adrenergic, dopamine).
Slower → Receptor Tyrosine Kinases (Minutes-Hours) → Phosphorylation cascades (e.g., insulin, EGFR).
Slowest → Nuclear Receptors (Hours) → Direct gene transcription (e.g., steroid hormones, thyroid hormones).
What medications are good for muskuloskeletal (MSK) pain but are less effective for neuropathic pain vs which medications are better for neuropathic pain
Diclofenac & tramadol work well for MSK pain (nociceptive pain) but are less effective for neuropathic pain.
Amitriptyline & pregabalin are first-line for neuropathic pain because they target abnormal nerve signaling
affinity
affinity= tenacity with which a drug binds to a receptor; determined by conc of drug required to occupy 50% of drug target at equilibrium (Kd)
what group of receptors do 5-HT receptors belong to
5-HT receptor are a group of G protein-coupled receptor
Define + give example of;
- full agonist
- partial agonist
- biased agonist
- inverse agonist
n.b.
affinity refers to the strength with which a ligand (such as a drug) binds to its receptor
efficacy denotes the ability of the ligand-receptor complex to produce a biological respons
full agonist (e.g. fentanyl (more potent), morphine, ropinirol)= has high efficacy, producing a full response while occupying a relatively low proportion of receptors
partial agonist (e.g. buprenorphine, varenicline)= have affinity for the receptor but low efficacy (can’t turn receptor on as much as full agonist)
biased agonist (e.g. TRV130/Oliceridine) or functionally selective agonists, preferentially activate specific signaling pathways over others through the same receptor (e.g. beta arrestin pathway instead of G-protein pathway
inverse agonist (e.g. Primavanserin used for parkinson’s psychosis)= opposite of an agonist so binds to receptor and induces negative efficacy (blocks it up basically)
Ropinirol
Ropinirol is a D2, D3 + D4 dopamine receptor agonist (highest affinity is for D2)
treats symptoms of Parkinson’s (stiffness, tremors, muscle spasms, poor muscle control) + restless legs syndrome
side effects:
dizziness when you get up from sitting or lying down.
feeling tired and weak.
stomach pain.
heartburn.
feeling sick or being sick.
feeling anxious or nervous.
uncontrollable twitching or twisting movements – this is more likely if you’ve been taking ropinirole for a long time or at a high dose.
Buprenorphine (aka Subutex)
Buprenorphine (aka Subutex)
- opioid receptor partial agonist GPCR
- produces pain relief with lower risk of respiratory depression
- used in situations of drug overdoes or opioid abuse
Varenicline (aka Chantix)
Varenicline (aka Chantix)
- alpha4/beta4 selective nicotinic receptor partial agonist (ligand-gated channel)
- used to treat nicotine dependence
TRV130/Oliceridine aka Olinvo
TRV130/Oliceridine aka Olinvo
is biased GPCR mu-opioid receptor agonist for moderate to severe pain
used for ppl with significant respiratory depression
still has some abuse and overdose potential and ability to produce opioid-dependence
what is a competitive vs non-competitive antagonist; give examples
Competitive antagonist= binds to same receptor as agonist. e.g. Propranolol
types of competitive antagonist:
- simple competitive
- pseudo-irreversible/ slowly dissociating
Non-competitive antagonist= Binds to a different site (allosteric site) or irreversibly to the receptor, preventing activation regardless of agonist concentration e.g. Ketamine NMDA receptor antagonist, binds non-competitively to prevent excitatory neurotransmission, used as an anesthetic and antidepressant.
types of non-competitive antagonists=
- irrevesible (chemically modifies receptor)
- allosteric
- functional: acts at second receptor
Name the type of agonist each of the following reversible competitive antagonists are blocking; also name the drug group + what it treats
- Ondansetron (aka Zofran)
- Carvedilol (Eucardic)
- Naloxone
Reversible competitive antagonists used to block endogenous agonist;
- Ondansetron (aka Zofran); 5-HT3 receptor reversible antagonist (of ligand-gated channel); used to inhibit vomiting (chemoradiotherapy)
- Carvedilol (Eucardic); beta1 adrenoreceptor reversible competitive antagonist (of GPCR); used in hypertension treatment
Reversible competitive antagonist used to block exogenous agonist;
- Naloxone; opioid receptor reversible competitive antagonist (of GPCR); used to reverse opioid-induced respiratory depression/ overdose
What is EC50
EC50 abbreviates for ‘half maximal effective concentration’= the concentration of a drug that is necessary to cause half of the maximum possible effect.
define
- pharmacokinetics
-pharmacodynamics
- pharmacokinetics; what the body does to the drug
-pharmacodynamics; what the drug does to the body
Grapefruit juice inhibits CYP3A4-mediated metabolism of medicines within small intestine; what drugs can you not drink grapefruit juice with? + What drugs are also CYP3A4 enzyme inhibitors
Drugs you can’t have graperfuit with: Cimetidine (H2 blocker), Omeprazole (proton-pump inhibitor), Statins
CYP3A4 enzyme inhibitors:
- protease inhibitors
- macrolide antibiotics
- fluoxetine
- cimetidine
- quinidine
- grapefruit juice
what is the first-pass effect in pharamacology (exhibited by propranolol)
The first-pass effect is a pharmacological phenomenon in which a medication undergoes metabolism at a specific location in the body. The first-pass effect decreases the active drug’s concentration upon reaching systemic circulation or its site of action
Define the following terms in pharmacokinetics;
- dose
- dosing interval
- Cmax
- Tmax
- Vol of distribution
- concentration
- elimination half life
- area under the curve
- clearance
- bioavailability
Dose = Amount of drug administered
Dosing interval = Time between drug dose administrations
Cmax = Peak plasma concentration of drug after administration
Tmax = Time to reach Cmax
Vol of distribution = Apparent volume in which drug is distributed (relates drug concentration in plasma to drug amount in the body)
Concentration = Amount of drug in a given volume of plasma
Elimination half-life = Time required for concentration of drug to reach half its original value
Area under the curve = Integral of the concentration-time curve (after a single dose or in steady state)
Clearance = Volume of plasma cleared of the drug per unit time
Bioavailability = The systemically available fraction of a drug
mechanism of action of Lamotrigine
Lamotrigine:
Mechanism of Action: Lamotrigine inhibits voltage-sensitive sodium channels, stabilizing neuronal membranes and modulating presynaptic transmitter release of excitatory amino acids.
mechanism of action of Ethosuximide
Ethosuximide:
Mechanism of Action: Ethosuximide’s exact mechanism is not entirely understood, but it most likely exerts its effects by partial antagonism of T-type calcium channels in thalamic neurons.
mechanism of action of Carbamazepine
Carbamazepine:
Mechanism of Action: Carbamazepine stabilizes sodium channels in their inactivated state, reducing the number of channels available to open. This prolongs the inactivated phase, inhibiting rapid and repetitive action potentials in the epileptic focus
mechanism of action of Sodium Valproate
Sodium Valproate:
Mechanism of Action: Sodium valproate increases gamma-aminobutyric acid (GABA) levels in the brain, enhancing its inhibitory effects. It also inhibits voltage-gated sodium channels and T-type calcium channels, reducing neuronal excitability
mechanism of action of Oxcarbazepine
Oxcarbazepine:
Mechanism of Action: Oxcarbazepine blocks voltage-sensitive sodium channels, stabilizing hyperexcited neuronal membranes and inhibiting repetitive neuronal firing.
mechanism of action of Levetiracetam
Levetiracetam binds to synaptic vesicle protein SV2A; inhibits presynaptic calcium channels; modulates neurotransmitter release
what are the major metabolites of morphine?
In man, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) are the major metabolites of morphine
difference between natural, synthetic and semi-synthetic opioids
Opiates, such as morphine and codeine, are natural opioids found in the opium poppy.
Synthetic opioids, such as methadone, are chemically made.
Heroin is a semi-synthetic opioid: it is made from morphine that has been chemically processed. It enters the brain quickly and produces a more immediate effect.
what is titration; up-titration vs down-titration
titrate means to gradually adjust the dose of a drug to achieve the desired therapeutic effect while minimizing side effects
Up-titration – Increasing the dose slowly until the desired effect is reached (e.g., adjusting beta-blockers in heart failure).
Down-titration – Gradually reducing the dose to avoid withdrawal effects (e.g., tapering corticosteroids or benzodiazepines).
what receptor does fentanyl work on
Fentanyl is a strong agonist of the μ-opioid receptor (mOR) (a class A GPCR)
what is the difference between analgesia vs anaesthetic
Analgesia is pain relief without loss of sensation or consciousness.
Anaesthesia, is loss of ALL physical sensation with or without loss of consciousness
