Drugs 3Rd Exam

Front 1

Donepezil (Aricept)

Back 1

Acetylcholinesterase inhibitor.
Treats all stages of AD.
Reversible inhibitor of AchE.
Long Half Life.
Few GI tract side effects.

Front 2

Rivastigmine (Exelon)

Back 2

AchE inhibitor.
Treats mild to moderate stages of AD.
More GI side effects than Donepezil (oral dosing).
Inhibition of AChE slowly reversible “PSEUDO IRREVERSIBLE”.
Patch Available.

Front 3

Galantamine (Razadyne)

Back 3

AchE inhibitor.
Treats miled to moderate stages of AD.
Reversible AchE inhibition.
May also have actions at Nicotinic receptors (clinical implications unknown).

Front 4

Tacrine (Cognex)

Back 4

liver toxicity, not generally used (FDA lists it as not
even being manufactured anymore!)

Front 5

Memantine (Namenda)

Back 5

Glutamate receptor partial antagonist to treat AD.
Treats moderate to severe AD.
An un-competitive (binds at Mg site), open channel
receptor antagonist with low to moderate affinity.
Voltage Dependent, Fast blocking and unblocking kinetics.
Usually given concomitantly with AChE inhibitor.

Front 6

Solanezumab

Back 6

Passive Immunotherapy for AD.
Antibody agains AB.
Ø Did not have efficacy in moderate to severe disease
Ø A hint of efficacy in mild disease
Ø Lilly will do bigger trial in mild disease
Ø Also a federally funded prevention study

Front 7

IntraVenous Immune Globulin (Gammaguard) therapy

Back 7

Ø antibodies are collected from the pooled blood of
thousands of donors
Ø FDA approved to treat certain conditions
Ø Phase III AD trial
Ø Cost- 5-10k/month

Front 8

Gingko Biloba

Back 8

Used as a dietary supplement.
Large, long term study found ginkgo did not reduce
the overall rate of dementia or AD incidence in elderly
individuals with normal cognition or MCI.
No effect on the rate of progression to dementia in
participants with MCI

Front 9

AN1792

Back 9

Stimulates own immune system to attack A(Beta) plaques
6% of patients developed meningoencephalopathy but 2/3 developed Antibodies.

Front 10

Chlorpromazine

Back 10

1st generation anti-psychotic.
Low potency.
Binding affinity to D2 only.
Doesn't dissociate antipsychotic action from EPS
Phenothiazines chemical family.
Chlorpromazine though carries a higher risk of other side effects such as sedation, anticholinergic effects and weight gain.
Can cause ocular deposits

Front 11

Haloperidol

Back 11

1st generation anti-psychotic.
High potency.
Binding affinity to D2 only.
Butyrophenones chemical family.
Haloperidol has higher potency and increased risk of EPS and hyperprolactinemia than does chlorpromazine.
Can cause ocular deposits.

Front 12

Clozapine

Back 12

2nd generation anti-psychotic.
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling
Has a lot of side effects.
Atypicals produce more weight gain and greater chance of metabolic issues than some typicals.
Can cause agranulocytosis (<2% of patients; weekly
blood counts for first 6 months, then every 3 weeks), seizures, myocarditis

Front 13

Olanzapine

Back 13

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling
Atypicals produce more weight gain and greater chance of metabolic issues than some typicals

Front 14

Quetiapine

Back 14

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling

Front 15

Risperidone

Back 15

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling
Risperidone has a risk of hyperprolactinemia at higher doses.

Front 16

Ziprasidone

Back 16

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling

Front 17

Aripiprazole

Back 17

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling
D2 partial agonist

Front 18

Asenapine

Back 18

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling

Front 19

Iloperidone

Back 19

2nd Generation Anti-psychotic
Tend to have a higher affinity for serotonin receptors than for dopamine receptors (efficacy and side effect profile)
● Tend to dissociate antipsychotic action from EPS
● Treat positive and maybe negative symptoms
● Hypothesized to even promote neuronal plasticity/remodeling

Front 20

Heroin

Back 20

Opioid.
Semisynthetic; diacetyl morphine.
Smoked, snorted and injected.
3x more potent than morphine.
Lipid soluble, intense rush when smoked or injected.

Front 21

Methadone (Demerol)

Back 21

Opioid.
Synthetic mu agonist; used to treat heroine addiction.
Long acting opiate used for analgesia and in treatment of opiate addicts. It is active after oral administration.
Long half life.

Front 22

Meperidine (Demerol)

Back 22

Opioid.
Synthetic, used widely in medicine, “new heroin”
Injected and Orally taken.
– 1/10th as potent as morphine
– Different side effects: including excitatory effects
such as tremors, delirium, hyperrelexia,
convulsions

Front 23

Fentanyl (sublimaze)

Back 23

Opioid.
Very lipid soluble; Fast acting
Injected.
Extremely short acting agent used mainly during anesthesia.
Found in transdermal skin patches and oral lozenges (“lollipops”).
80-500 X potency of morphine
Illicit use: "China White"

Front 24

Morphine

Back 24

Most potent drug in opium
Comprises 10% of crude extract
Injected.
Mu agonist.
Used mainly for post-operative pain, due to reasonably long duration of action.

Front 25

Codeine

Back 25

Most commonly used drug worldwide today.
Less potent; comprises .5%
Injected and Oral.
Low efficacy opiate that is used widely for cough suppression and for minor pain.

Front 26

Opium

Back 26

Extract of opium poppy.
Smoked and injected

Front 27

Naltrexone

Back 27

Opioid receptor antagonist.
Used in treatment for treating heroin addicts.

Front 28

Pentazocine (Talwin)

Back 28

Mixed Agonist-Antagonist
Produce an agonist effect at one receptor and an antagonistic effect at another. Clinically useful mixed drugs are kappa agonists and mu antagonists. Display ceiling effect for analgesia (decreased efficacy)

Front 29

Buprenorphine (Buprenex)

Back 29

Partial Agonist bind receptors but with low intrinsic activity.
Binds all three opioid receptors but with lower
efficacy.

Front 30

Naloxone (Narcone)

Back 30

Prototype opiate antagonist. Main clinical use is to treat opiate overdose.
Displaces morphine from mu R and blocks analgesia.

Front 31

Remifentanyl

Back 31

10-20 minute half-life; IV to
control brief, intense pain during surgery

Front 32

Oxycodone

Back 32

• Oral agent used to treat pain
• Abuse is increasingly common
• Preventative measure: slow release
formulation that reduces utility of crushed
pills and limits the “rush” of euphoria

Front 33

Tramadol

Back 33

Partial agonist opioid; reduced addiction risk

Front 34

Dezocine (Dalgan)

Back 34

Mixed agonist-antagonist opioids; reduced addiction risk

Front 35

Nalbuphine (Nubain)

Back 35

Mixed agonist-antagonist opioid; reduced addiction risk

Front 36

Butorphanol (Stadol)

Back 36

Mixed agonist-antagonist opioid; reduced addiction risk