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HHD5 pharmacology, Flumazenil is an ANTAGONIST, blocks benzodiazepines and…

- - - - zolpidem
    - - suvorexant
    - - Melatonin
  - - - Buspirone
  - - - Barbituate
        
        Secobarbitol
      - benzodiazepine
        
        midazolam and triazolam
      - Ethanol
        
        Alcohol
    - - antihistamine
        
        diphenhydramine
- - - - lorazepam and clonazepam
        
        Anticonvulsant benzodiazepines (GABAr agonists), clonazepam for acute seizures & epilepsy in kids (myclonic, Lennox-Gastaut) while lorazepam i.v. is for status epilepticus; but tolerance develops to either drug
    - - Ethosuximide
        
        Anticonvulsant, low-threshold (T-type) Ca++ Channel Blocker, for only absence seizures
      - Phenytoin & Fosphenytoin
        
        Anticonvulsant (Na Channel blocker), oral phenytoin is for partial & tonic-clonic seizures, while i.v. prodrug fosphenytoin (which slowly converts to phenytoin) is a first-line drug for status epilepticus; numerous adverse-Fx (Tx, drug-drug, teratogenic)
      - Broad Spectrum
        
        Lamotrigine
        
        Anticonvulsant, broad spectrum (due to triple mechanisms), 1st-line anticonvulsant in pregnancy; also used broadly due to favorable side-Fx profile (except for significant risk of skin rash, rarely progressing to Stevens-Johnson Syndrome [SJS] skin necrosis)
        
        Levetiracetam
        
        Anticonvulsant, broad spectrum, binds & inhibits SV2A synaptic vesicle glycoprotein, inhibiting presynaptic calcium release; because it is effective, has safe side-Fx profile, and no drug interactions, is a VERY commonly-prescribed anticonvulsant
  - - - Carbamazepine
        
        Anticonvulsant Na+ Channel Blocker, for simple & complex partial seizures; also for neuropathic pain and bipolar depression; induces CYP3A; increased risk of Steven-Johnsons Syndrome [SJS] skin necrosis in some HLA genotypes (pharmacogenetics
      - Gabapentin & Pregabalin
        
        Anticonvulsant presynaptic voltage-dependent (VDCC) Ca++ Channel Blocker, for partial seizures, neuropathic pain, and Restless Leg Syndrome [RLS]
      - Cannabidiol [CBD]
        
        Anticonvulsant antiglutamatergic (anadamide metabolism blocker & inhibitory CB1 & Glycine Receptor agonist), for Dravet & Lennox-Gastaut syndromes, also for neuralgia
      - Divalproex [Valproic Acid]
        
        Anticonvulsant AND Migraine drug, for broad-spectrum seizures & for preventing migraine, also for bipolar disorder, multiple mechanisms (inhibits GABA metab;blocks Na+ and T-type Ca++ Channels), IQ teratogen
      - Topiramate
        
        Anticonvulsant AND Migraine drug, for partial & generalized seizures (incuding Lennox-Gastaut syndrome) & for preventing migraine, also for alcoholism, multiple mechanisms (Na+ Channel Blocker, GABA agonist, Glu AMPA inhibitor), cleft-palate teratogen
  - - - subcutaneous injection
        
        OnabotulinumtoxinA
        
        Migraine drug, for preventing migraine (trigeminal nerve-transported neuroinhibitor), paralysis or death if incorrectly injected
      - Erenumab
      - tricyclic antidepressant
        
        Amitriptyline
      - beta-blocker (blood pressure medication)
        
        propranolol
      - Selective serotonin receptor agonists
        
        sumatriptan
- - - - Selective Serotonin Reuptake Inhibitor
        
        fluoxetine
        
        side effects include initial anxiety/suicide risk, sexual dysfunction (anorgasmia)
    - - MAOI Monoamine Oxidase Inhibitors
        
        Phenelzine
        
        antidepressant, MAO inhibitor, serious drug & food interactions
    - - Tricyclic antidepressant
        
        amitriptyline
        
        1stGen SNRIs -- inhibits 5HT (serotonin) & NE (norepinephrine) reuptake), AND neuralgia (Na-channel blocker) & migraine drug; TCAs have severe anticholinergic & antiadrenergic side-effects, serotonin syndrome + MAOIs, potentiate sedatives
    - - atypical
        
        bupropion
        
        antidepressant, atypical, inhibits DA & NE re-uptake (DNRI), used to treat nicotine addiction, no sexual side effects
      - glutamatergic
        
        Low-dose ketamine
        
        antidepressant, glutamatergic, activates AMPA glutamate receptors, instant antidepressant effect, lasts +2wks
      - multimodal serotonergic
        
        vortioxetine
        
        inhibits 5HT (serotonin) reuptake PLUS affects multiple 5HT (serotonin) receptor subtypes including 5HT7 antagonist (procognitive), minimal side effects
    - - Serotonin and Norepinephrine Reuptake Inhibitor
        
        venlafaxine
        
        antidepressant, SNRI, side-effects milder than TCAs, but includes hypertension
  - - - lithium
        
        side effects weakness, thirst, Low therapeutic index (can get toxic on higher doses), NSAIDs toxicity
    - - carbamazepine
        
        Na+ Channel Blocker, also for simple & complex partial seizures and neuropathic pain, induces CYP3A; increased risk of Steven-Johnsons Syndrome [SJS] skin necrosis in some HLA genotypes (pharmacogenetics
    - - cariprazine
        
        bipolar antidepressant (mood stabilizer) and atypical antipsychotic, partial D2 antagonist, motor side effects
- - - - Valbenazine
        
        Tardive Dyskinesia
        
        Drug for Tardive Dyskinesia (TD); VMAT2 inhibitor; reduces DA release to compensate for D2 supersensitization
      - Tetrabenazine
        
        Huntington's Disease
        
        Drug for Huntington's Disease (HD); VMAT2 inhibitor, depletes DA; PD-like, depression, cardiac risks
      - Levodopa
        
        Dopamine (DA) precursor, metabolized to DA in brain (and, unfortunately, peripherally as well)
      - Carbidopa
        
        Blocks peripheral metabolism of levodopa to DA, allowing more levodopa to enter brain
      - Levodopa+Carbidopa = Sinemet
        
        2-drug combination for DA replacement therapy, for Parkinson's Disease [PD] (see above)
      - Entacapone
        
        COMT inhibitor. Blocks peripheral metabolism of levodopa to an inactive metabolite
      - Trihexyphenidyl
        
        anticholinergic drug for PD (inhibits motion-suppressing neurons); most useful in early-stage PD (elderly patients can't handle anticholinergic SLUD side-Fx well) and for PD tremors
      - Ropinirole
        
        DA D3>D2 agonist for PD, non-ergoline class (no fibrosis), also used for RLS
      - Amantadine
        
        Enhances DA release from remaining undegenerated Substantia Nigra afferents, and blocks GLU, for PD.
      - Selegiline
        
        MAO-B inhibitor of brain DA's metabolism to DOPAC, for PD. Antidepressant interaction (serotonin syndrome); metabolized to amphetamine
  - - - 1x daily
        
        1x daily Reversible Cholinesterase Inhibitor (Cholinomimetic), for Alzheimer's Disease (AD), liver-Tx drug interactions
        
        2x daily
        
        2x daily Reversible Cholinesterase Inhibitor (Cholinomimetic) for AD, no liver-Tx or Tx drug interactions
        
        3x daily
        
        3x daily Reversible Cholinesterase Inhibitor (Cholinomimetic) & potentiates Nicotinic AchR, for AD.
    - - Memantine
        
        NMDAr antagonist for AD, blocks low-level chronic GLU neurotoxicity but allows pulsatile GLU for learning
- - - - Partial agonist
        
        Buprenorphine
        
        partial µ-agonist for opioid addiction (partial = antagonist with heroin AND agonist during withdrawal, limited euphoria itself), also for analgesia
      - CNS Antagonist
        
        Naloxone
        
        µ-antagonist, short half-life, for opioid OD rescue; also not effective orally, so added to oral buprenorphine to prevent patient abusing buprenorphine by i.v. or snorting
      - Long half life agonist
        
        Methadone
        
        long-lived µ-agonist for opioid addiction (long half-life = blocks heroin effects AND withdrawal), take in clinic to avoid abusing it
    - - Treat Diarrhea
        
        Loperamide
        
        enteric nervous system-specific µ-agonist, use for reducing diarrhea (gut motility), would have to eat a truck load of this to get high.
      - Treat Opioid Constipation
        
        Methylnaltrexone
        
        peripheral nervous system-specific (i.e., enteric nervous system plus peripheral nociceptor neuron) µ-antagonist, use for relieving constipation in chronic opioid-treated patients; can counteract opioids' peripheral nociceptor analgesia
  - - - Codeine
        
        less potent µ-opioid receptor agonist than (but metabolized to) morphine, for throat pain w/ cough suppressant
    - - Fentanyl, carfentanil, remifentanil
        
        super-potent µ-opioid receptor agonists compared to other opioids (fentanyl 100x more potent than morphine, used as patch that is abused by chewing; carfentanil 10,000x used to sedate elephants; remifentanil 20,000x but short half-life, used i.v. for labor)
    - - Oxycodone
        
        more potent µ-opioid receptor agonist than morphine, slow-release coating (abused by chewing pills)
    - - Meperidine
        
        stimulating µ-opioid receptor agonist with added SNRI properties, for short-term analgesia with less CNS depression (but risk of Serotonin Syndrome drug interaction with MAO inhibitors or SSRIs)
    - - Morphine
        
        µ-opioid receptor agonist, analgesic & drug of abuse
      - Heroin
        
        faster-acting µ-opioid receptor agonist than morphine (more lipid/blood-brain-barrier soluble)