Drugs And Their Actions Exam 2, Drugs To Know

Front 1

Diazepam (Valium®)

Back 1

Benzodiazepine, Treats anxiety, long acting agent

Front 2

Chlordiazepoxide (Librium®)

Back 2

Benzodiazepine, Treats anxiety, long acting agent

Front 3

Clonazepam (Klonopin®)

Back 3

Benzodiazepine, Treats anxiety, intermediate acting agent

Front 4

Lorazepam (Ativan®)

Back 4

Benzodiazepine, Treats anxiety, intermediate acting agent

Front 5

Triazolam (Halcion®)

Back 5

Benzodiazepine, Treats anxiety, short acting agent

Front 6

Alprazolam (Xanax®)

Back 6

Benzodiazepine, Treats anxiety, short acting agent

Front 7

Flumazenil (Romazicon®)

Back 7

Benzodiazepine receptor antagonist.
● Binds to benzodiazepine receptor with high affinity but produces no effect on GABA signaling (doesn’t do much on its own)
● Reverses the antianxiety and sedative effects of
benzodiazepines
● Short half-life
● Utilized as a benzodiazepine antidote

Front 8

Zolpidem (Ambien®)

Back 8

Non-Benzodiazepine receptor agonists, used to treat insomnia

Front 9

Zaleplon (Sonata®)

Back 9

Nonbenzodiazepine BZRA, short term treatment for insomnia

Front 10

Eszopiclone (Lunestra®)

Back 10

Nonbenzodiazepine BZRA, longest half life/best treatment for insomnia

Front 11

Ramelteon (Rozerem®)

Back 11

Melatonin Receptor agonist

Front 12

Buspirone (BuSpar®)

Back 12

Serotonin receptor agonist, Antianxiety, SSRI

Front 13

Disulfram (Antabuse)

Back 13

Reduce Alcohol relapse.
An alcohol sensitizing drug
Mechanism of action(s):
1) Inhibit aldehyde
dehydrogenase
2) Also may work by
Modulating neurotransmitters
involved in addiction
End result: alcohol ingestion causes build up of acetaldehyde
Efficacy of disulfiram for treatment of alcoholism has been called into question- may have utility in treating cocaine dependence

Front 14

Naltrexone (ReVia, Vivitrol)

Back 14

Reduce Alcohol relapse.
Goal: Reduce craving for alcohol
Mechanism of action: opioid antagonist, thought that
reinforcing properties of alcohol involve opioid systems
Effects are small, but issue with non-compliance
Evidence that genetics may influence efficacy
Vivitrol- extended release, injectable naltrexone

Front 15

Acamprosate (Campral)

Back 15

Reduce Alcohol relapse.
Thought to restore balance of GABA/glutamate
neurotransmission
Mechanism of action: thought to have GABA-agonistic
action and an inhibitory action at NMDA receptors

Front 16

Imipramine (Tofrenil®)

Back 16

TCA,

Front 17

Trazodone (Desyrel®)

Back 17

2nd Generation anti-depressant, Priapism is a huge side effect

Front 18

fluoxetine-olanzapine (Symbyax®)

Back 18

SSRI combo that treats bipolar disorder

Front 19

Venlafaxine (Effexor®)

Back 19

Dual action antidepressant

Front 20

Duloxetine (Cymbalta®)

Back 20

Dual action antidepressant, most effective

Front 21

Bupropion (Welbutrin®)

Back 21

Dual action antidepressant, Dopamine-Norepinephrine reuptake inhibitor (DNRI) (Only one)
- blocks uptake of dopamine (strongly);
norepinephrine and serotonin (weakly)
- antagonism of certain nicotinic receptors
- in a study using bupropion treatment for 8
weeks, 30% were smoke-free a year later (16%
of patch users were)

Front 22

Varenicline (Chantix)

Back 22

- binds more weakly to receptor than does
nicotine
- prevents access of nicotine to receptor
- what is the end pharmacologic effect?
- Increases chances of quitting and
maintaining abstinence for a year 3 fold
(placebo) or 1.5 fold (bupropion)
- Not used in conjunction with nicotine
replacement

Front 23

flunitrazepam (Rohypnol®)

Back 23

Benzodiazepine.
● Date rape drug with strong amnesic properties
● Street slang = Roofie

Front 24

Methaqualone (Quaalude)

Back 24

● Highly abused in the 1980s
● Served as an early date rape drug since it had
amnesic properties
● It is now banned from sale

Front 25

Chloral Hydrate (Noctec)

Back 25

● It is rapidly metabolized to trichloroethanol
● Added to alcohol it forms a “Mickey Finn”: an early date rape
mixture causing amnesia

Front 26

GAMMA HYDROXYBUTYRATE (GHB) (XYREM)

Back 26

In some countries used as anesthetic
Used to treat narcolepsy (Xyrem)
Sedative/hypnotic Abused
Used as a “date rape” drug
Adverse effects include toxicity, seizures, respiratory depression, vomiting. Toxicity magnified by alcohol.

Front 27

Imipramine (Tofrenil®)

Back 27

TCA.
w Block presynaptic norepinephrine and serotonin
reuptake transporters
w Block postsynaptic histamine, acetylcholine and
norepinephrine receptors
Side Effects:
w Anticholinergic activity can lead to confusion, memory
and cognitive impairment, dry mouth, blurred vision,
increased heart rate, and urinary retention
w Antihistaminic activity can cause drowsiness and
sedation
w Antiadrenergic effects can cause postural hypotension
w Life-threatening effects are a concern, especially for
overdose in a patient population that may consider
suicide
● Cardiac effects like arrythmias
● Excitement and convulsions
● Respiratory depression and coma

Front 28

phenelzine (Nardil®)

Back 28

w Drugs are inhibitors of monoamine oxidases
● MAO-A metabolizes dopamine, norepinephrine
and serotonin
● These antidepressants inhibit this form causing
neurotransmitter build-up
● MAO-B metabolizes dopamine
w Three MAOIs have been used to treat major
depressive illnesses
Side Effects:
w MAOIs cause serious side effects with certain foods
and medicines
w In addition to therapeutic action on neurotransmitters,
MAOIs inhibit tyramine metabolism
w Tyramine is at significant levels in several foods
including cheese, wine, beer, liver, some beans,
fermented and/or pickled sauces and vegetables,
cured and/or aged meats, others
w Tyramine increases blood pressure
w Eating a high tyramine food like cheese while taking a
MAOI drug can easily raise systolic blood pressure
30mm-HG or more
w In extreme cases, ingesting tyramine containing foods
while taking MAOIs can cause an “adrenergic storm”
causing extreme tachycardia, extreme hypertension,
and possibly death
w MAOIs also have drug interactions with some nasal
sprays, antiasthma and cold medicines

Front 29

Trazodone (Desyrel®)

Back 29

2nd Generation Antidepressant.
Mechanism of action
- Does not block the reuptake of norepinephrine or
serotonin
- Trazodone blocks 5-HT2 receptors
- Its metabolite m-chlorophenylpiperazine is a
serotonin agonist
Side Effects:
- Drowsiness is most common
- Priapism is a rare but more serious side effect
- Priapism requires surgery in about 33% of cases
and can cause permanent impotence
- Trazodone has only modest effects on cognitive
functioning even with overdoses

Front 30

fluoxetine (Prozac®)

Back 30

SSRI, LEAST selective for 5-HT
w Mechanism of Action
Ÿ All act as serotonin reuptake inhibitors
Ÿ Some also act as norepinephrine reuptake blockers
Ÿ These agents vary greatly (12-fold) in their ability to
block norepinephrine reuptake
w Side Effects
Ÿ Very few anticholinergic and antihistaminic
effects except for fluoxetine which is very
sedating
Ÿ These drugs are not fatal in overdose
(No cardiac toxicity like TCAs)

Front 31

paroxetine (Paxil®)

Back 31

SSRI, Most implicated in causing Serotonin Syndrome
w Mechanism of Action
Ÿ All act as serotonin reuptake inhibitors
Ÿ Some also act as norepinephrine reuptake blockers
Ÿ These agents vary greatly (12-fold) in their ability to
block norepinephrine reuptake
w Side Effects
Ÿ Very few anticholinergic and antihistaminic
effects except for fluoxetine which is very
sedating
Ÿ These drugs are not fatal in overdose
(No cardiac toxicity like TCAs)

Front 32

sertraline (Zoloft®)

Back 32

SSRI
w Mechanism of Action
Ÿ All act as serotonin reuptake inhibitors
Ÿ Some also act as norepinephrine reuptake blockers
Ÿ These agents vary greatly (12-fold) in their ability to
block norepinephrine reuptake
w Side Effects
Ÿ Very few anticholinergic and antihistaminic
effects except for fluoxetine which is very
sedating
Ÿ These drugs are not fatal in overdose
(No cardiac toxicity like TCAs)

Front 33

fluvoxamine (Luvox®)

Back 33

SSRI
w Mechanism of Action
Ÿ All act as serotonin reuptake inhibitors
Ÿ Some also act as norepinephrine reuptake blockers
Ÿ These agents vary greatly (12-fold) in their ability to
block norepinephrine reuptake
w Side Effects
Ÿ Very few anticholinergic and antihistaminic
effects except for fluoxetine which is very
sedating
Ÿ These drugs are not fatal in overdose
(No cardiac toxicity like TCAs)

Front 34

citalopram (Celexa®)

Back 34

SSRI, MOST selective for 5-HT
w Mechanism of Action
Ÿ All act as serotonin reuptake inhibitors
Ÿ Some also act as norepinephrine reuptake blockers
Ÿ These agents vary greatly (12-fold) in their ability to
block norepinephrine reuptake
w Side Effects
Ÿ Very few anticholinergic and antihistaminic
effects except for fluoxetine which is very
sedating
Ÿ These drugs are not fatal in overdose
(No cardiac toxicity like TCAs)

Front 35

escitalopram (Lexapro®)

Back 35

SSRI
w Mechanism of Action
Ÿ All act as serotonin reuptake inhibitors
Ÿ Some also act as norepinephrine reuptake blockers
Ÿ These agents vary greatly (12-fold) in their ability to
block norepinephrine reuptake
w Side Effects
Ÿ Very few anticholinergic and antihistaminic
effects except for fluoxetine which is very
sedating
Ÿ These drugs are not fatal in overdose
(No cardiac toxicity like TCAs)

Front 36

fluoxetine-olanzapine combination (Symbyax®)

Back 36

SSRI combo used to treat bi-polar disorder

Front 37

Venlafaxine (Effexor®)

Back 37

Dual-Action Antidepressant.
inhibits both serotonin and
norepinephrine reuptake
w Inhibits serotonin reuptake at lower doses
w No anticholinergic and antihistaminic effects
w Comparable efficacy to imipramine in treating OCD
side effects of concern
Ÿ Sexual dysfunction
Ÿ Increases blood pressure in a low percentage of
patients
Ÿ Possibly more toxic in overdose than other
SSRIs

Front 38

Duloxetine (Cymbalta®)

Back 38

seems to have more complete
blockade of reuptake systems than venlafaxine
w Also appears to reduce headache, backache, muscle
and joint pain
w Approved for the management of neuropathic pain of diabetic peripheral neuropathy
w Most prevalent side effects are nausea, dizziness,
and dry mouth

Front 39

Bupropion (Welbutrin®), Antidepressant info

Back 39

Dual Action Antidepressant.
is the only dopamine-
norepinephrine reuptake inhibitor (DNRI)
w Does not affect serotonin reuptake so it does not have
the side effects of SSRIs
w Dopamine potentiation is used to treat children with
ADHD
w Produces effects of minimal sexual dysfunction or
enhanced sexual functioning
Side Effects:
may result in weight loss
w Bupropion general side effects include anxiety,
restlessness, tremor and insomnia
w Bupropion serious side effects include psychosis and seizures
w Bupropion has a mechanism like cocaine but it is not generally abused