Block 3 Drugs Flashcards by Beth Stinchcombe

Dopaminergics

Pharmacology of Basal Ganglia Disorders

Levodopa (L-dopa)

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Levodopa (L-dopa) MoA

Dopamine precursor

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Dopaminergics

Pharmacology of Basal Ganglia Disorders

Pramipexole

Ropinirole

Rotigotine

Apomorphine

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Dopaminergics (Pramipexole / Ropinirole / Rotigotine / Apomorphine) MoA

Dopamine D2 receptor agonist (synthetic)

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Dopa-decarboxylase inhibitor

Pharmacology of Basal Ganglia Disorders

Benserazide

Carbidopa

(Car - Benz - Dope)

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Dopa-decarboxylase inhibitor MoA

Stops breakdown of Levadopa in periphery by inhibiting dopa-decarboxylase

(Can be given in combo with L-dopa)

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COMT (catechol-O-methyl transferase) Inhibitor

Pharmacology of Basal Ganglia Disorders

Entacapone

Tolcapone

(Big guns when nothing else working - Al Capone)

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COMT (catechol-O-methyl transferase) Inhibitor MoA

Stops breakdown of dopamine in CNS by inhibition of COMT

Used in later stages of disease

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MAOB (monoamine oxidase, B form) Inhibitor

Pharmacology of Basal Ganglia Disorders

Selegiline

Rasagiline

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MAOB (monoamine oxidase, B form) Inhibitor MoA

Stops breakdown of dopamine into homovanillic acid in CNS by inhibition of MAOIB

(Better for younger patients in which motor symptoms are not impacting QoL, can be used with as an adjunct with L-dopa in later stages)

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Anticholinergics

Pharmacology of Basal Ganglia Disorders

Procyclidine

Orphenadrine

Trihexphenidyl

(POT = CRAzy muscles)

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Anticholinergics MoA

Muscarinic cholinergic receptor antagonist

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Anti-Parkinsonism

Pharmacology of Basal Ganglia Disorders

Amantadine

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Anti-Parkinsonism MoA

Antiviral - glutamate (NMDA) receptor antagonist, dopamine agonist

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Dopamine-depleting drugs

Pharmacology of Basal Ganglia Disorders

Tetrabenazine

Playing Tetris depletes phone battery

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Dopamine-depleting drugs MoA

Blocks VMAT, preventing uptake of dopamine into vesicles - used for hyperkinetic movement disorders

(Playing Tetris depletes phone battery)

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Weak Analgesic/Antipyretic

Analgesic Drugs

Paracetamol

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Weak Analgesic/Antipyretic MoA

Non-selective COX inhibitor (CNS)

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Non-steroidal anti-inflammatory drugs (NSAIDs)

Analgesic Drugs

Aspirin

Ibuprofen

Diclofenac

Naproxen

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Non-steroidal anti-inflammatory drugs (NSAIDs) MoA

Analgesic Drugs

Non-selective COX inhibitor

Non-selective COX inhibitor blocks enzyme action of platelet COX enzyme.
COX is required for synthesis of thromboxane A2 (TXA2).
Reduced TXA2 inhibits platelet activation and thrombus formation.

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COX2-selective NSAIDs

Analgesic Drugs

Celecoxib

Etoricoxib

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COX2-selective NSAIDs MoA

Analgesic Drugs

Selective COX-2 inhibitor

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Weak Opioid Analgesics

Analgesic Drugs

Codeine

Dihydrocodeine

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Weak Opioid Analgesics MoA

Analgesic Drugs

Opioid receptor agonist

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Weak Opioid Analgesics: Side Effects | Analgesic Drugs

Nausea Vomiting Light-headedness Dizziness Sweating Constipation

Strong Opioid Analgesics | Analgesic Drugs

Morphine (half life 3/4 hrs) Diamorphine (half life 3/4 hrs) Methadone (long half-life over 24 hrs) Fentanyl (short half-life 1/2 hrs)

Strong Opioid Analgesics MoA | Analgesic Drugs

Opioid receptor agonist

Partial/Mixed Agonist-Antagonist Opioid Analgesic | Analgesic Drugs

Buprenophine (half-life 12 hours)

Partial/Mixed Agonist-Antagonist Opioid Analgesic MoA | Analgesic Drugs

Opioid receptor agonist (μ)/antagonist (κ)

Opioid Receptor Antagonist | Analgesic Drugs

Naloxone (short half life - 1/2 hours) Naltrexone (long half life - 10 hours)

Opioid Receptor Antagonist MoA | Analgesic Drugs

Opioid receptor antagonist

Synthetic Opioid | Analgesic Drugs

Tramadol

Synthetic Opioid MoA | Analgesic Drugs

Opioid receptor agonist + 5HT/NA reuptake inhibitor

Drugs to Manage Opioid Addiction | Analgesic Drugs

Methadone Buprenorphine

Drugs Treat Neuropathic Pain | Analgesic Drugs

Tricyclic Antidepressants (TCAs) - see TCA cards Gabapentin (AED) - MoA: inhibits VDCC, increases GABA transmission Pregabalin (AED) - MoA: inhibits VDCC, Carbamazepine (AED) - MoA: sodium channel blocker

Tricyclic Antidepressants (TCAs) | Pharmacology of Depression

Amitriptyline (also used for neuropathic pain) Nortriptyline (also used for neuropathic pain) Clomipramine (also used for neuropathic pain)

Tricyclic Antidepressants (TCAs) MoA | Pharmacology of Depression

SRI, NRI, H1, M1, noradrenaline a1 Adrenergic antagonist

Selective serotonin reuptake inhibitors (SSRIs) | Pharmacology of Depression

Sertraline Citalopram (good for older patients) Escitalopram

Selective serotonin reuptake inhibitors (SSRIs) MoA | Pharmacology of Depression

Inhibits serotonin (5HT) reuptake pump N.B side effect: can have increase in negative symptoms e.g. suicidal intention before mood improves and serotonin syndrome: hyperthermia, CV problems, aggression, tremor and rigidity -> MEDICAL EMERGENCY!

Monoamine (A) oxidase inhibitors (MAOIs) | Pharmacology of Depression

Moclobemide

Monoamine (A) oxidase inhibitors (MAOIs) MoA | Pharmacology of Depression

Stops breakdown of monoamines in CNS. Reversible inhibitor of monoamine oxidase A (RIMA)

Monoamine (A) oxidase inhibitors (MAOIs): Side Effect | Pharmacology of Depression

Tyramine cheese reaction -> vasoconstriction and hypertension = MEDICAL EMERGENCY! Do not use with SSRIs/TCA's!

Atypical Antidepressant | Pharmacology of Depression

Venlafaxine

Atypical Antidepressant: Venlafaxine MoA

SNRI

Atypical Antidepressant | Pharmacology of Depression

Reboxetine

Atypical Antidepressant: Reboxetine MoA

NRI

Atypical Antidepressant | Pharmacology of Depression

Bupropion

Atypical Antidepressant: Bupropion MoA

NDRI

Atypical Antidepressant | Pharmacology of Depression

Mirtazapine

Atypical Antidepressant: Mirtazapine MoA

α2-Adrenergic antagonist

1st Generation Antipsychotic

Chlorpromazine Haloperidol

1st Generation Antipsychotic MoA

Selective dopamine (D2) receptor antagonist

2nd Generation Antipsychotic

Risperidone (used in PTSD) Clozapine

2nd Generation Antipsychotic MoA

Serotonin (5HT2A) + dopamine (D2) antagonist | can also be used for disorders of the basal ganglia

3rd Generation Antipsychotic

Aripiprazole | last resort - RIP

3rd Generation Antipsychotic MoA

Partial agonist at 5HT and DA receptors

Anxiolytic - anxiety drug (adjunct in depression) | Anxiolyics and Related Drugs

Buspirone

Anxiolytic - anxiety drug (adjunct in depression) MoA | Anxiolyics and Related Drugs

5HT1a partial agonist

Muscle relaxants / Sedatives / Anxiolytic-hypnotic | Anxiolyics and Related Drugs

SSRI/SNRI

SSRI/SNRI MoA

5HT1a partial agonist

Muscle relaxants / Sedatives / Anxiolytic-hypnotic | Anxiolyics and Related Drugs

Zolpidem ('Z-drug') | uses: short term/crises

Zolpidem ('Z-drug') MoA | Anxiolyics and Related Drugs

GABA PAM (γ-subunit) (mechanistically identical to BDZ)

Muscle relaxants / Sedatives / Anxiolytic-hypnotic | Anxiolyics and Related Drugs

Temazepam

Temazepam MoA | Anxiolyics and Related Drugs

GABA PAM (γ-subunit) (mechanistically identical to BDZ)

Symptom Reduction (Autonomic) | Anxiolyics and Related Drugs

Propranolol | uses: specific phobia to reduce symptoms only

Symptom Reduction (Autonomic) MoA | Anxiolyics and Related Drugs

β-blocker aka β-adrenegic receptor

Anti-epilepsy drugs (AEDs)

Sodium valproate (Side effect: anti-epileptic hypersensitivity syndrome / TERATOGENIC) Lamotrigine (First line for epilepsy apart from generalised tonic-clonic) Ethosuximide (First line for generalised absence) Carbemazepine (Side effect: anti-epileptic hypersensitivity syndrome)

Sodium valproate / Lamotrigine / Carbemazepine MoA

Sodium channel blocker

Ethosuximide MoA

Calcium channel blocker (T-type)

Benzodiazepine (BDZ) | Epilepsy Drugs

Midazolam Lorazepam (uses: epilepsy and anxiety - short term/crises) Diazepam

Benzodiazepines (BDZ) MoA | Epilepsy Drugs

GABA PAM (γ-subunit)

BDZ Antagonist | Epilepsy Drugs

Flumazenil

BDZ Antagonist MoA | Epilepsy Drugs

Competitive antagonist at BDZ site

Barbiturates | Epilepsy Drugs

Phenobarbitone Pentobarbitone Primidone

Barbiturates MoA | Epilepsy Drugs

GABA PAM (β-subunit)

Adjuncts | Epilepsy Drugs

Tiagabin Levetiracetam

Adjuncts MoA | Epilepsy Drugs

Tiagabin - GABA reuptake inhibitor Levetiracetam - unclear

Anticholinesterases | Drugs used for Dementia

Donepezil Galantamine Rivastigmine

Anticholinesterases MoA | Drugs used for Dementia

Inhibitor of acetylcholinesterase (reversible)

Glutamate (NMDA) receptor antagonists | Drugs used for Dementia

Memantine

Glutamate (NMDA) receptor antagonists MoA | Drugs used for Dementia

VD blocker of NMDA (N-Methyl-D-aspartate) receptor

Antimicrobial drugs | Drugs used for CNS infection

Ceftriaxone (antibiotics, B4)

Ceftriaxone MoA | Drugs used for CNS infection

Inhibits synthesis of cell walls in bacteria

Antimicrobial drugs | Drugs used for CNS infection

Amoxicillin (antibiotics, B4)

Amoxicillin MoA | Drugs used for CNS infection

Induces cell lysis by blocking last stages of cell wall synthesis

Corticosteroid

Dexamethasone

Corticosteroid MoA

Glucocorticoid receptor agonist