Block Three Bolded Drugs Flashcards
Amitryptyline
Tricyclic antidepressant for chronic pain
Non-specific - blocks 5HT and NE reuptake
Atypical antipsychotic
- Clozapine
- Olanzapine
- Resperidone
- Quetiapine
- Aripiprazole
Decreased incidence of extrapyramidal symptoms, improved negative symptoms.
B-endorphine
Endogenous opioid peptide.
In hypothalamus and nucleus tractus solitarius. Also in anterior pituitary co-released with ACTH during stress.
B-endorphin
Endogenous opioid peptide.
In hypothalamus and nucleus tractus solitarius. Also in anterior pituitary co-released with ACTH during stress.
Buprenorphine
Partial Mu agonist
25-50x more potent than morphine
Treats moderate to severe pain.
Bupropion
Atypical antidepressant
Weakly blocks NE and DA uptake
Also approved for nicotine withdrawl and seasonal affective disorder.
Chlorpromazine
A typical antipsychotic
Clozapine
Atypical antipsychotic
Blocks D4 and 5HT receptors, little effects on D2, muscarinic antagonist
Decreases seizure threshold
Can cause fatal agranulocytosis
Codeine
Opioid agonist for mild pain.
Some metabolized to morhpine
Sometimes used with aspirin and acetaminophen
Duloxetine
SNRI
Half-life 12-18 hours
Used for neuropathic pain, fibromyalgia, back pain, osteoarthritis.
Caution pts with liver disease,.
Withdrawl symptoms.
Dynorphin
Endogenous opioid peptide
Localized with vasopressin in hypothalamus and posterior pituitary.
Shorter ones have wide CNS distribution.
Enkephalin
Endogenous opioid peptide
Leu and Met enkephalins have wide CNS distribution
Found in periphery in adrenal medulla, nerve plexuses, and exocrine glands of the stomach and intestines.
Fentanyl
Mu agonist
100x more potent than morphine, short acting: 1-1.5 hrs.
Buccal, injectable, and transdermal
Fluoxetine
SSRI
Adverse effects: insomnia, sexual dysfunction, nausea.
Long half life (7+ days)
Approved to treat PMDD
Haloperidol
typical antipsychotic
Heroin
Diacetyl morphine
More lipophilic than morphine, converted to 6-acetyl morphine and morphine
Hydrocodone
Opioid agonist for moderate to severe pain
Available in sustained release oral preparation
Hydromorphone
2-3x more potent than morphine
Levorphanol
Affinity at Mu receptor (most), Delta, and Kappa.
5HT/NE reuptake inhibitor, NMDA antagonist.
Rapid onset.
Major Depressive Disorder
5 or more symptoms for 2+ weeks-one of which must be depressed mood or loss of pleasure in doing things.
weight change, insomnia/hypersomnia, feeling worthless, suicidal ideation, fatigue
Monoamine oxidase inhibitor
Block oxidative deamination of biogenic amines (NE, DA, 5HT) A form associated with antidepressant action
Can cause hypomania in bipolar.
Treats major depression and narcolepsy.
Meperidine
Opioid agonist, shorter DOA than morphine.
Forms toxic metabolite: normeperidine than can accumulate
Interacts with MAOIs
Mesocortical pathway
Starts A10
Functions in cognition, communication, and social activity.
Change in dopaminergic activity causes negative symptoms.
Mesolimbic pathway
Starts at A10
Functions in arousal, stimulus processing, locomotor activity, and motivational behavior.
Dopamine hyperactivity causes positive symptoms.
Methadone
Opioid agonist with good oral F, long duration of action
Treatment of opioid abuse and chronic pain
Mirtazapine
Atypical antidepressant that blocks presynaptic alpha2 receptors in brain
Used to increase appetite in AIDs patients
Morphine
Mu agonist with low oral to parenteral potency (F=~.3)
4-5 hr analgesia
Nalbuphine
Mixed agonist
Similar in efficacy to morphine
Can cause withdrawl symptoms in opioid dependent pts
Injection only
Naloxone
Opioid receptor antagonist with high Mu affinity and less for delta and kappa receptors.
DOA = 1-2 hrs
Naltrexone
Opioid antagonist with long half life (24+ hours)
Treats alcoholism and opioid addiction
Olanzapine
Atypical antipsychotic
5HT, D1, D2 antagonist with some effect on D4
Decreased seizures compared to clozapine, and no agranulocytosis.
Causes weight gain and diabetes.
Oxycodone
Opioid agonist for moderate to severe pain
Available in sustained release oral preparation
Pentazocine
Mixed agonist, effective doses often yield similar effects as full Mu agonists
Phenelzine
Irreversible MAO inhibitor
Psychosis
Derangement of personality, loss of contact with reality, delusions, hallucinations
Quetiapine
Atypical antipsychotic
Similar to olanzapine and clozapine in treating symptoms and side effects
Decreased half life. Approved for augmentation in depression.
Resperidone
Atypical antipsychotic prodrug
D2 and 5HT antagonist
Greater decrease in negative symptoms and less extrapyramidal symptoms
Less seizures and less antimuscarinic effects.
Intramuscular injection
Schizophrenia
2 or more symptoms for one month (one being a core positive):
Core +: delusions, hallucinations, disorganized speech
Negative: blunted affect, poverty of thought, decreased cognitive ability, social withdrawl
Sertraline
SSRI
Adverse effects: nausea, insomnia, sexual dysfunction
Shorter half life than fluoxetine, decreased impact on drug metabolism.
Treats OCD, PTSD, and panic attacks.
SNRI
Blocks 5HT and NE reuptake.
Side effects more SSRI-like than TCA-like
Suboxone
Oral buprenorphine with naloxone to treat opioid dependence.
Tramadol
Weak Mu agonist blocks NE and 5HT uptake
Used for moderate pain
Tricyclic Antidepressants
Block NE and 5HT reuptake.
Treats neuropathic pain and depressive disorders.
“Dirty” drug
- binds H1 to cause sedation
- Binds muscarinic receptors to cause blurred vision, constipation, and glaucoma
- Binds alpha adrenergic receptors to cause hypotension, dixzziness, and reflex tachy.
8-100 hr half life.
Alprazolam
Benzodiazepine; treats anxiety
Baclofen
Binds GABA B receptor and increases GABA’s ability to bind, resulting in an increase in Cl- moving into the cell and thus hyperpolarization and inhibition.
Muscle relaxant; just as effective as diazepam with less sedation.
Benzodiazepines
Bind GABA receptor and increase GABA’s ability to bind, thereby increasing the amount of Cl- moving into the cell causing hyperpolarization and inhibition.
Result is relaxation and sleep.
Buspirone
Partial 5HT1A agonist
Inhibits adenylate cyclane and opens K+ channels; also binds dopamine receptors
Treats generalized anxiety disorder
Chlordiazepoxide
Benzodiazepine with long half-life used to treat alcohol withdrawal.
Diazepam
Benzodiazepine; increases GABAs ability to bind its receptor resulting in more Cl- into the cell and hyperpolarization.
Muscle relaxant/hypnotic at high doses.
Divalproex
Antiseizure agent, 1st line for Bipolar I.
Blocks Na+ channels and may increase synaptic GABA.
Sedating.
Flumazenil
Antagonist at benzodiazepine receptor.
Can treat benzo OD or reverse benzos post-op.
Flurazepam
Benzodiazepine; rapid onset with long duration of action.
Metabolized to active metabolite: desalkylflurazepam
Lamotrigine
Antiseizure agent
Blobks Na+ channels
Can be used to treat bipolar I
Lithium
Monovalent cation
Blocks manic behavior
Blocks the progression of IP2 -X—> IP so phosphoinositol can’t be recycled in the IP3 and DAG 2nd messenger system.
Lorazepam
Benzodiazepine; treats anxiety and insomnia
Tizanidine
Skeletal muscle relaxant
alpha2 adrenergic agonist related to clonidine
Enhances pre and postsynaptic transmission; causes drowsiness, hypotension, and asthenia (weakness).
Valproic Acid
Antiseizure agent, 1st line for bipolar I
Blocks Na+ channels and may increase synaptic GABA.
Sedating.
Zolpidem
Non-benzodiazepine that blocks the benzodiazepine receptor on GABA receptor complex.
Increases GABAs ability to bind its receptors.
Primarily used for sleep.
Acamprosate
GABA-A agonist thought to normalize dysregulated neurotransmission and decrease drinking frequency and relapse in abstinent pts.
Alcohol dehydrogenase (ADH)
Converts ethanol into acetaldehyde using a lot of NAD+
Converts Methanol to formaldehyde.
Women have lower amounts of this enzyme than men.
Aldehyde dehydrogenase
Converts acetaldehyde to acetate in ethanol metabolism. using NAD+.
Converts Formaldehyde to formate in methanol metabolism.
Amphetamine
Potentiates NE, DA, and 5HT signaling at the trace amine associated receptor (TAAR1) to inhibit reuptake AND cause reversal (release of amines) from terminal and vesicles.
Beriberi
Thiamine deficiency from chronic alcohol abuse
“dry”: peripheral neuropathy, wernicke’s aphasia, and korsakoff’s psychosis.
“wet”: CV presentation
Caffeine
Methylxanthine similar in structure to purines.
Competitive antagonist at adenosine receptor.
Clonidine
Alpha2 adrenergic receptor agonist used to treat ADHD (not a stimulant).
Disulfiram
Can block aldehyde dehydrogenase to treat ethylene glycol poisoning.
Can be used for aversion therapy, results in accumulation of acetaldehyde which is very uncomfortable.
Ethanol
Alcohol
Can be used to block alcohol dehydrogenase in methanol poisoning.
Ethylene glycol
Metabolized by alcohol dehydrogenase and aldehyde dehydrogenase
Fomepizole
Can be used to block alcohol dehydrogenase in methanol poisoning.
Guanfacine
Alpha2 adrenergic receptor agonist used to treat ADHD (not a stimulant)
Methamphetamine
Potentiates NE, DA, and 5HT signaling at the trace amine associated receptor (TAAR1) to inhibit reuptake AND cause reversal (release of amines) from terminal and vesicles.
Methanol
Metabolized by alcohol dehydrogenase and aldehyde dehydrogenase to toxic metabolites formaldehyde and formate.
Methylphenidate
Not an amphetamine, but structurally and mechanistically very similar.
Microsomal Ethanol Oxidizing System
Cytochrome P450 2E1, 1A2, 3A4 used to metabolize ethanol to acetaldehyde using NADPH.
2E1 is induced in alcoholics and increases clearance of other drugs.
Nicotine
Agonist of nicotinic cholinergic receptors.
CNS stimulant causing alertness, increases DA release in reward centers, muscle relaxant, and activates chemoreceptor trigger zone to cause nausea (w/ first exposure).
Thiamine
Deficiency associated with alcohol abuse, can cause beriberi
Varenicline
Partial agonist of nicotinic receptors
Reduces nicotine craving by activating nAChR.
More efficacious than placebo and buproprion at 12 and 24 wks.
Benzocaine
Ester local anesthetic that is applied to wounds and ulcerations for longer relief of pain.
Bupivicaine
Amide local anesthetic
Long acting; provides more sensory than motor relief. More cardiotoxic than lidocaine.
Desflurane
Volatile liquid for outpatient surgeries and maintenance of anesthesia.
Not used for induction because of respiratory irritation.
Etomidate
Induces anesthesia in patients at risk for hypotension
Pain on injection, myoclonus, nausea and vomiting. Suppresses adrenocortical stress response (bad).
Isoflurane
Moderate blood:gas partition coefficient
Most common inhaled anesthetic; airway irritant that causes coughing.
Ketamine
Dissociative anesthesia
NMDA receptor antagonist
Bronchodilator
Lidocaine
Local amide anesthetic
Faster, more intense, and longer lasting than procaine.
Midazolam
GABA-A agonist.
Short-acting benzodiazepine used for conscious sedation
Nitrous oxide
Weak anesthetic used for sedation and analgesia at 50% concentration.
Often combined with other anesthetics or used for dental work.
Procaine
Ester local anesthetic
Short acting, low potency, slow onset.
Propofol
Uses GABA-A mechanism to induce and maintain anesthesia.
Most commonly used general anesthetic in the US.
Ropivacaine
S-enantiomer, long acting amide local anesthetic.
Actions like bupivocaine with less cardiotoxicity.
Used for epidural and regional anesthesia.
Sevoflurane
Gaseous anesthetic used for induction and maintenance.
NOT a respiratory irritant; less respiratory depression than other gaseous anesthetics.
Sodium thiopental
Barbiturate that acts through GABA-A receptor to induce anesthesia within 10-30 seconds after IV infusion of a single dose.
Lasts 10 minutes tops.
Not used in the US, used to be used for lethal injection.
Tetracaine
Local ester anesthetic
Long acting, more potent and longer duration of action than procaine.
Used for spinal anesthesia and ophthalmic use.
