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Narcotic-Analgesics (opioids) (act on, uses)
-mimic endogenous opioids (endorphins and enkephalins, neuropeptides produced in CNS and pituitary gland)
-Uses: anesthetics for surgery, pain/analgesic
-methadone only is used for opioid UD (reduces cravings + withdrawal sxs)
Natural and synthetic/semi-synthetic opioids (names)
Natural: opium, heroin, codeine, morphine
Synthetic/semi-synthetic: oxy/hydrocodone, methadone, fentanyl
Methadone (uses, acts on)
-synthetic opioid for opioid UD and treatment-resistant severe pain
-direct opioid agonist (mimicking endorphins + enkephalins) at Mu-opioid receptors
-NMDA receptor antagonist (blocks glutamate, dampens excitatory pain pathways)
-inhibits S and N reuptake
Side effects of narcotic-analgesics
-respiratory depresssion
-pupil constriction, postural hypotension
-constipation
(think opioids have CNS depressant effect, can’t breathe, see, or poop)
Sudden withdrawal from opioids →
-flu-like sxs (initial 24 hrs): yawning, runny nose, watery eyes, muscle aches, fever
-later: high BP, high HR, GI distress (cramps, diarrhea, vomiting)
Opioid overdose leads to
convulsions, coma, death
Two psychedelics that are labeled FDA ‘breakthrough’ drugs
Form of LSD: for GAD
serotonin agonist, and increases dopamine
Psilocybin: for MDD, treatment-resistant depression
serotonin agonist, and increases glutamate (neuroplasticity)
Benzos + barbituates (act on)
-increase GABA
Benzodiazepines (names, uses, which ones have slightly longer half-life)
Uses:
-anxiety/insomnia
-seizures (CNS depressant)
-alcohol withdrawal (similar CNS depressant effects as alcohol)
-Diazepam (Valium)
-Alprazolam (Xanax) and Lorazepam (Ativan) – shorter HL, need longer taper
Benzodiazepine withdrawal can be
-life-threatening (withdrawal seizures, delirium, rebound anxiety/depression)
(sudden stopping of GABA inhibition → hyperexcitability)
Barbituate withdrawal can be
FATAL (barbituates are stronger than benzos)
-seizures, delirium, death
(sudden stopping of GABA inhibition → hyperexcitability)
Benzos + barbituates cannot be taken with…
-Alcohol (can be lethal)
-Some high BP medications (→ dangerous drop in BP)
Benzodiazepine Side Effects
(Too much slowing + possible paradoxical effect, esp. in children and older adults)
-sedation + weakness/unsteadiness + cognitive slowing
-anticholinergic effects, sexual dysfunction
-in older adults, benzos process slower (72 instead of 24 hrs): SEs of disorientation/confusion
-paradoxical effect = excitability + anxiety (in children and older adults)
Barbituates Side Effects
(same as benzos + ataxia – even more severe unsteadiness/poor balance)
-sedation + ataxia + cognitive slowing
-paradoxical excitement
Barbituates (names, uses)
-thiopental (Pentothal)
-amobarbital (Amytal), secobarbital (Seconal)
Uses:
-anxiety/insomnia
-seizures
-general anesthetic (even more depressant than benzos)
Azapirone (Buspirone) (use, side effects)
-GAD and other anxiety disorders
-advantage of buspirone: doesn’t cause sedation or dependence/tolerance
-SEs: nausea/dizziness, some initial drowsiness (but not same sedative effects as benzos/barbituates), dry mouth, sweating, headache
Beta blockers/propanolol (act on, uses)
-block SNS activity (epinephrine + norepinephrine)
Uses:
-high BP, heart arrythmias
-essential tremor
-migraine headache
-physiological anxiety
Beta blockers side effects
-low BP
-depression, dry eyes, decreased sex drive
-insomnia
Suddenly stopping beta blockers →
-rebound sxs of all the things it treats (suddenly stopped blocking adrenaline) → high BP, arrhythmia tremors, headaches, confusion
Mood stabilizers for bipolar (which drugs, their names)
1.) Lithium
2.) Anticonvulsants: carbamazepine + valproic acid (for mixed episodes, acute mania)
Why is regular blood testing needed for lithium, carbamazepine, and valproic acid?
Lithium: lithium toxicity (seizures, coma, death)
Carbamazepine: agranulocytocis (extremely low WBC count) + aplastic anemia (bone marrow unable to produce all 3 types of blood cells), and liver failure
Valproic acid: liver failure
Side effects of lithium
-metallic taste, increased thirst (think: to rid of the metal taste)
-hand tremor
-weight gain (ppl don’t like being on lithium)
Lithium pts shake, drink, and gain weight
Anticonvulsant Side Effects
-sedation (sleepy, lethargic)
-ataxia, tremor (unsteady)
-visual disturbances, impaired concentration
Alzheimer’s disease drugs (what type of drugs)
1.) Cholinesterase inhibitors (increase ACh, by blocking cholinesterase enzyme that breaks down ACh)
2.) NMDA receptor antagonists (blocks glutamate) – Memantine, approved for moderate to severe Alzheimer’s
Cholinesterase inhibitors for Alzheimer’s (names)
-Donepezil – only one approved for severe Alzheimer’s
-Tacrine – risk of liver failure and serious SEs, no longer prescribed
-Galantamine
-Rivastigmine
Stimulants (act on, names, additional info)
-increases dopamine + norepinerphrine in PFC (same as bupropion)
-Pemoline (Cylert)
-Methylphenidate (Ritalin, Concerta), Amphetamine-dextroamphetamine (Adderall)
-concern about growth suppression in children––reversible with drug holidays in summers
-in ppl w/o ADHD: increases attention + positive mood (NOT reading comprehension + fluency); worsens WM and academic performance
Other ADHD Medications (prescribed with comorbid tic disorder)
-Atomexetine (Strattera): Norepinephrine reuptake inhibitor; also for sleep and anxiety/depression
-Guanfacine + Clonidine: alpha-2-adrenergic agonists, originally high BP meds (regulates Norepinephrine)
Antidepressants used with ADHD
-desipramine (TCA, secondary amine, Norpramin)
-bupropion (NDRI)
Alcohol use disorder drugs
-Disulfiram (Antabuse) = Deterrent (violent vomiting, throbbing headache, fast HR)
-Naltrexone and Topiramate – targets cravings + pleasurable effects
-Acamprosate – reduces cravings, doesn’t target pleasurable effects of alcohol
Topiramate (Topamax)
-an anti-seizure medication; not FDA-approved for alcohol UD
-Uses: alcohol UD, some evidence for cocaine UD
-reduces cravings + pleasurable effects of alcohol (just like Naltrexone)
Tobacco use disorder drugs
-Nicotine replacement therapy (stable low level nicotine reduces withdrawal sxs that lead to relapse)
-Varenicline – reduces craving + rewarding effects
-Bupropion – reduces cravings + withdrawal sxs
Cocaine Use Disorder drugs
-No FDA approved drugs
-some evidence for bupropion, topiramate, and some psychostimulants (modafinil, dextroamphetamine, mixed amphetamine salts)
TetraHydroCannabinol (THC, acts on)
-main active ingredient of cannabis
-stimulates release of Dopamine in ventral striatum (nucleus accumbens), an essential part of the mesolimbic pathway (dopaminergic reward system)
Dronabinol oral solution (Syndros, uses)
(Think THC munchies)
-For anorexia/appetite and weight loss in AIDS
-and nausea/vomiting in chemotherapy pts
Two FDA-approved psychedelic drugs: form of LSD and Psilocybin (uses, act on)
-both serotonin agonists (think Peter’s depression)
-form of LSD – for GAD; also increases dopamine
-Psilocybin – for MDD, treatment-resistant depression; also regulates glutamate
Half-life of drugs in older adults
e.g., benzos with longer HL are eliminated in 24 hrs; but 72 hrs in older adults
“Go low and slow”
Cross-tolerance
e.g., tolerance to alcohol → tolerance to benzos + barbituates (all CNS depressants)
-tolerance to 1 drug produces tolerance in other drugs of same class
Therapeutic index (TI)
-measures drug’s safety
-ratio of lethal/toxic dose to effective dose
LD50/ED50 or TX50/ED50
Wide vs. narrow therapeutic window
-We want BIG TIs, wide therapeutic windows (TI > 1.0)
-narrow therapeutic window = lethal/toxic dose is ≥ the effective dose (not safe, requires close monitoring)