Drugs

Question 1

Agonist

Answer 1

Function – drug effect that mimics or increase the effects of a neurotransmitter.

Question 2

Partial Agonist

Answer 2

Function – drug effect that produces a similar, yet weaker effect of a neurotransmitter.

Question 3

Inverse Agonist

Answer 3

Function – drug effect that produces the opposite effect of a neurotransmitter.

Question 4

Antagonist

Answer 4

Function – drug effect that blocks or reduces the effect of a neurotransmitter or agonist.

Question 5

First Gen Antipsychotics
FGA

Answer 5

Function – treat schizophrenia & other psychotic symptoms; typical/traditional; block dopamine receptors (D2)

Chemicals – +dopamine

Drugs –
* Chlorpromazine/Thorazine
* Haloperidol/Haldol
* Thioridazine/Mellaril
* Fluphenazine/ Piloxin

Side Effects –
* anticholinergic
* extrapyramidal
* neuroleptic malignant syndrome

Question 6

Anticholinergic Side Effect

Answer 6

Function – drug side effect; from low potency FGA

Drugs –
* Chlorpromazine/Thorazine
* Thioridazine/Mellaril

Symptoms –
* dry mouth
* blurred vision
* urinary retention, constipation
* tachycardia (fast heartrate)
* confusion, impaired attention/concentration

Question 7

Extrapyramidal Side Effect

Answer 7

Function – drug side effect; from high potency FGA

Drugs –
* Haloperidol/Haldol
* Fluphenazine/ Piloxin

Symptoms –
* parkinsonism (resting tremor, muscle rigidity, slowed movement)
* dystonia (uncontrollable muscle contractions, head/neck)
* akathisia (inner restlessness)
* tardive dyskinesia (starts with involuntary, rhythmic movements of tongue/face/jaw, progresses to limbs/trunk) after long-term FGA use, potentially fatal, common in women, older adults; irreversible, but treated with withdrawal of FGA + -dopamine, +GABA SGA or benzodiazepine.

movement related issues & sensations

Question 8

Neuroleptic Malignant Syndrome

Answer 8

Function – rare drug side effect

Symptoms –
* muscle rigidity
* high fever
* autonomic dysfunction (unstable blood pressure, tachycardia, excessive sweating)
* altered mental sate (combativeness, confusion)
* treated with withdrawal of FGA + supportive therapy (cooling/hydration) + medical treatment

Question 9

Second Gen Antipsychotics
SGA

Answer 9

Function – treat schizophrenia, bipolar, & other psychotic symptoms; atypical; as or more effective for treating positive symptoms + more effective for treating negative symptoms; some are FDA-approved to treat depressive disorders; block dopamine receptors (D3+D4) for negative symptoms + block serotonin receptors for cognitive symptoms.

Chemicals – +dopamine, +serotonin

Drugs –
* Clozapine/Clozaril
* Risperidone/ Risperdal
* Olanzapine/Zyprexa
* Quetiapine/Seroquel
* Aripiprazole/Abilify

Side Effects –
* likely to cause extrapyramidal (Clozapine/Clozaril)
* metabolic syndrome (weight gain, insulin resistance, hyperglycemia, diabetes mellitus)
* agranulocytosis (Clozapine/Clozaril; life threatening low white blood cell count)
* less likely than FGA to cause anticholinergic + neuroleptic malignant syndrome

Question 10

SSRI
selective serotonin reuptake inhibitor

Answer 10

Function – treat depression; first-line pharmacological treatment; also treats premenstrual dysphoric disorder, panic disorder, OCD, GAD, bulimia, & premature ejaculation.

Chemicals – +serotonin

Drugs –
* Fluoxetine/Prozac
* Fluvoxamine/Luvox
* Paroxetine/Paxil
* Sertraline/Zoloft
* Citalopram/Celexa

Side Effects –
* mild anticholinergic effects
* gastrointestinal disturbance, headache (tummy hurt, head hurt)
* insomnia, anxiety, sexual dysfunction
* tachycardia, antidepressant intolerance (poop-out; apathy, fatigue)
* abrupt cessation of the SSRI causes discontinuation syndrome (headaches, dizziness, mood liability, poor sleep + concentration, flu-like symptoms)
* serotonin syndrome when mixed with MAOIs

extra- fewer SE + o/d safer than TCA; safer for older adults;

Question 11

SNRI

Answer 11

Function – treat depression, anxiety, neuropathic pain, & other pain disorders;

Chemicals – +serotonin, +norepinephrine

Drugs –
* Venlafaxine/Effexor
* Duloxetine/Cymbalta
* Desvenlafaxine/Pristiq

Side Effects –
* discontinuation syndrome
* serotonin syndrome (potentially fatal extreme confusions, agitation, autonomic instability, hyperthermia, tremors, seizures, delirium) treated with immediate withdrawal of SNRI + medical treatment
* anticholinergic effects
* insomnia, headaches, sexual dysfunction
* not good for hypertension + heart problems because of norepinephrine

Question 12

NDRI

Answer 12

Function – treat major depression & smoking cessation;

Chemicals – +norepinephrine, +dopamine

Drugs –
* Bupropion/Wellbutrin/Zyban

Side Effects –
* anticholinergic effects
* energic effects (so not useful for anxiety)
* skin rash, low appetite, weight loss, agitation, insomnia, dizziness, seizures
* no sexual dysfunction; no cardiotoxicity

Question 13

TCA
tricyclic antidepressants

Answer 13

Function – treats depression, anxiety, OCD, panic, neuropathic pain; includes secondary amines (more norepinephrine than serotonin; less side effects) & tertiary amines (more serotonin than norepinephrine)

Chemicals – +serotonin, +norepinephrine, +dopamine

Drugs –
secondary
* Nortriptyline/Pamelor
* Desipramine/Norpramin
tertiary
* Amitriptyline/Elavil
* Impramine/Tofranil
* Clomipramine/Anafranil
* Doxepin/Sinequan

Side Effects –
* anticholinergic effects
* cardiovascular effects (hypertension, tachycardia, * orthostatic hypotension)
* sedation, weight gain, sexual dysfunction

+extra- lethal in overdose; must be prescribed with caution for patients with SI/heart disease

Question 14

MAOI
monoamine oxidase inhibitors

Answer 14

Function – monoamine oxidase inhibitors; works to increase the chemical trio by inhibiting monoamine oxidase enzyme from removing those chemicals from the brain; treats atypical/treatment-resistant depression (hypersomnia, increase appetite, reactive dysphoria, reactive mood, leaden paralysis, rejection sensitivity).

Chemicals – +serotonin, +norepinephrine, +dopamine

Drugs –
* Phenelzine/Nordi
* Isocarboxazid/Marplan
* Tranylcypromine/Parnate

Side Effects –
* daytime sleepiness, insomnia, sedation, sexual dysfunction
* orthostatic hypotension
* anticholinergic effects
* hypertensive crisis (fatal autonomic symptoms + confusions, delirium, light sensitivity) can occur when taken with amphetamines, antihistamines, and tyramine foods (aged cheese/meat, soy, beer/wine, banana)
* tachycardia, antidepressant intolerance (poop-out; apathy, fatigue)
* serotonin syndrome when mixed with SSRIs

Question 15

Lithium

Answer 15

Function – mood stabilizer; treats bipolar disorder; first-line drugs for euphoric mania without rapid cycling; levels must be checked to avoid lithium-toxicity, seizures, coma, death.

Chemicals – +serotonin, +norepinephrine, +dopamine, +glutamate

Drugs –
* Lithium/Lithobid/Eskalith
Side Effects –
* nausea, vomiting, diarrhea
* metallic taste, increased thirst, weight gain
* hand tremor, fatigue
* impaired memory/concentration

Question 16

Anticonvulsant Drugs

Answer 16

Function – mood stabilizer; treats acute mania + bipolar with mixed episodes; levels must be checked to avoid liver failure.

Chemicals – +serotonin, +norepinephrine, +dopamine, +glutamate

Drugs –
* Valproic Acid/Depakene
* Carbamazepine/Tegretol (levels must be checked to avoid agranulocytosis, low white-blood cells, + aplastic anemia, bone marrow fails to make new blood cells)

Side Effects –
* nausea, dizziness
* sleepiness, lethargy
* ataxia, tremor, visual disturbances
* impaired concentration

Question 17

Psychoactive Drugs

Answer 17

Function – treat anxiety, insomnia, seizures; includes sedatives, hypnotics, and anxiolytics; includes benzodiazepines, barbiturates, and azapirones; discontinuation must be tapered.

Side Effects –
* drowsiness, confusion
* tolerance, dependence, + withdrawal symptoms with chronic use
* combined with alcohol can be lethal

Question 18

Benzodiazepines

Answer 18

Function – psychoactive drug; treats anxiety, insomnia, seizures, & alcohol withdrawal; discontinuation must be tapered (ex: long use with a short half-life required a longer taper)

Chemical – +GABA

Drugs –
* Diazepam/Valium
* Alprazolam/Xanax (short half-life)
* Lorazepam/Ativan (short half-life)

Side Effects –
* drowsiness, sedation, weakness
* impaired memory/concentration (disorientation/confusion in older adults)
* anticholinergic effects
* sexual dysfunction
* tolerance, dependence, + withdrawal symptoms with chronic use
* combined with alcohol, causes lethal synergistic depressant effects
* combined with high blood pressure meds (alpha blockers/central agonists), causes a dangerous drop in blood pressure

Question 19

Barbiturates

Answer 19

Function – psychoactive drug; treats anxiety, insomnia, & seizures; discontinuation must be tapered

Chemical – +GABA

Drugs –
* Thiopental/Pentothal
* Amobarbital/Amytal
* Secobarbital/Seconal

Side Effects –
* drowsiness, dizziness, confusion
* ataxia, cognitive impairment, paradoxical excitement
* tolerance, dependence, + withdrawal symptoms with chronic use
* seizures, delirium, death with sudden withdrawal
* combined with alcohol, causes lethal synergistic depressant effects

Question 20

Azapirones

Answer 20

Function – psychoactive drug; treat anxiety disorders

Chemical – +GABA

Drugs –
* Buspirone/BuSpar

Side Effects –
* dizziness, headaches
* dry mouth, nausea
* no dependence, tolerance, or sedation effects

Question 21

Narcotic-Analgesics (Opioids)

Answer 21

Function – treat pain + used for pre-surgery anesthetics;

Chemical – mimics endorphins + enkephalins

Drugs –
* Natural Opioids (opium, morphine, heroin, codeine)
* Synthetic/Semi-synthetic Opioids (methadone, oxycodone, hydrocodone, fentanyl)

Side Effects –
* dizziness, drowsiness
* constipation, dry mouth, nausea
* pupil constriction, respiratory depression
* tolerance, dependence, + withdrawal symptoms (flu-like) with chronic use
* overdose causes convulsions, coma, death

*extra- methadone used to treat heroin detox because it reduces withdrawal symptoms + cravings without pleasurable effects

*extra- drug overdose is the #1 cause of US deaths; opioids are the most frequent cause of these deaths

Question 22

Beta Blockers

Answer 22

Function – treats somatic anxiety symptoms, hypertension, cardiac arrythmias, migraines, & tremors; inhibit sympathetic nervous system activity; sudden cessation can cause rebound symptoms of hypertension, cardiac arrythmias, and confusion.

Drugs –
* Propranolol/Inderal

Side Effects –
* dizziness, drowsiness
* dry mouth & eyes, nausea, vomiting
* insomnia, depression, decreased libido
* hypotension

Question 23

Alzheimer’s Drugs

Answer 23

Function – slows Alzheimer’s progression; cholinesterase inhibitors (delay the breakdown of acetylcholine) & NMDA receptor antagonists (regulating glutamate activity).

Chemical - +glutamate, +ACE

Drugs –
cholinesterase (mild-severe)
* Tacrine/Cognex (risk of liver failure, not often prescribed)
* Donepezil/Aricept (severe)
* Rivastigmine/Exelon
* Galantamine/Razadyne
NMDA (moderate-severe)
* Memantine/Namenda

Question 24

Psychostimulants for ADHD

Answer 24

Function – first-line treatment for ADHD; increase attention/concentration, reduce hyperactivity/impulsivity

Location – prefrontal cortex

Chemical - +dopamine, +norepinephrine

Drugs –
* Methylphenidate/Ritalin/Concerta
* Pemoline/Cylert
* Amphetamine-Dextroamphetamine/Adderall

Side Effects – reversable with cessation
* insomnia, decreased appetite, weight loss
* abdominal pain, nervousness
* suppress growth in children

Question 25

Other Drugs for ADHD

Answer 25

Function – second/third-line treatment for ADHD when poor response to psychostimulants; increase attention/concentration, reduce hyperactivity/impulsivity

Chemical - +norepinephrine (Atomoxetine/Strattera, Tricyclic/Norpramin, Bupropion/Wellbutrin), +alpha-2-adrenergic (Guanfacine/Intuniv, Clonidine/Kapvay), +dopamine (Tricyclic/Norpramin, Bupropion/Wellbutrin)

Drugs –
second line
* Atomoxetine/Strattera (most prescribed non-stim + more effective for comorbidities)
* Guanfacine/Intuniv (good for hypertension; only for Tourette’s/tic disorder comorbidity)
* Clonidine/Kapvay (good for hypertension; only for Tourette’s/tic disorder comorbidity)
third line (antidepressants)
* TCA Desipramine/Norpramin
* NDRI Bupropion/Wellbutrin

Question 26

Drugs for Alcohol Use Disorder

Answer 26

Function – treats alcohol use disorder

Drugs –
* Disulfiram/Antabuse
Side Effects – nausea, vomiting, headache, dizziness, shortness of breath, tachycardia

• Naltrexone/ReVia
  Side Effects – reduces drug pleasure + cravings
• Acamprosate/Campral
  Side Effects – reduces drug cravings
• Topiramate/Topamax (anti-seizure med; not DFA for alcohol disorder treatment)
  Side Effects – reduces drug pleasure + cravings

Question 27

Drugs for Tobacco Use Disorder

Answer 27

Function – treats tobacco use disorder

Drugs –
* Nicotine replacement therapy (NRT; works by tapering nicotine levels)
* Bupropion/Wellbutrin (antidepressant; reduces cravings + withdrawal)
* Varenicline/Chantix (reduces cravings + drug reward effects

Question 28

Drugs for Cocaine Use Disorder

Answer 28

No FDA-approved drug treatments

Drugs –
Bupropion/Wellbutrin, Topiramate/Topamax, and other psychostimulants (Modafinil, Adderall, amphetamine salts) may be effective in increasing abstinence

Question 29

Tetrahydrocannabinol
THC

Answer 29

Function – active ingredient in cannabis; psychoactive effects be increasing dopamine in the ventral striatum (mesolimbic dopaminergic pathway).

Drugs –
* Dronabinol oral solution/Syndros (FDA approved for weightless issues, anorexia, AIDS, chemo)

Question 30

Therapeutic Index

Answer 30

Function – drug safety measure; animal & human studies; when ED50 equals LD/TD50, TI ≤ 0.1 is said to have a narrow therapeutic window, which are not safe because the does that produces the desired effect is close to the toxic/lethal dose. TI > 1 is said to have a wide therapeutic window, most desirable because safer.

Animal Studies –
* LD50 (minimum amount for a lethal dose in 50% of the sample) divided by ED50 (minimum effective dose in 50% of the sample)

Human Studies –
* TD50 (minimum amount for a toxic dose in 50% of the sample) divided by ED50 (minimum effective dose in 50% of the sample)