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BMB > Exam 6 (drugs only) > Flashcards

Exam 6 (drugs only) Flashcards

1
Q

Tx for acute MS relapse

A

High dose IV methylprednisolone = 1 mg

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2
Q

2 disease modifying drugs used to tx MS

  • MoA
  • side effects
  • reduction in relapse rate
  • administration routes
A
  1. Beta-interferon
    - MoA - inhibits pro-inflammatory cytokines, T-cell proliferation, CNS trafficking
    - Side effects - myalgia and chills
    - Administered - subq and IM
    - broad impact on inflammation
  2. Glatiramer acetate
    - mixture of amino acids
    - similar efficacy and side effects as above
    - give SQ

BOTH - 30 to 40% reduction in relapse rate

BOTH - tx relapsing remitting and 2ndary progressive MS

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3
Q

What 2 drugs are more effective than beta-interferon and glatiramer acetate for txing relapsing remitting and 2ndary progressive MS?

  • MoA
  • side effects
  • administration route
A

NATALIZUMAB

  1. MoA
    - binds to integrin-cellular adhesion molecule
    - blocks lymphocytes-endothelial binding which prevents cell from crossing BBB
  2. Administered through IV monthly
  3. Side effects -> PML in 0.2%

FINGOLIMOD

  1. MoA
    - blocks egress of lymphocytes from lymph nodes and spleen
  2. Administered orally (unique)
  3. Side effects
    - risk of heart block in some w/ initial dose ONLY
    - 1 case of PML reported
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4
Q

2 other oral agents to tx MS

A

dimethyl fumarate and teriflunomide

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5
Q

List 2 anticholinergic medications discussed in the dementia lecture

A

Benztropine (Cogentin)

Trihexyphenidyl (Artane)

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6
Q

List 2 medications with anticholinergic action

A

Amitriptyline (Elavil)

Diphenyhydramine (Benadryl)

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7
Q

Tx for absence epilepsy

  • include dosing
  • standard and atypical
A
  • Ethosuximide 20 mg/kg/day: Standard

* Valproic Acid 20 mg/kg/day: If atypical

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8
Q

Major DA systems in the CNS

  • highest concentration of DA found in which pathway?
  • which one is the therapeutic target of antipsychotics?
  • side effects
A
  1. Nigrostriatal
    - SN to corpus striatum
    - majority of DA here
    - SIDE EFFECT -> EPS (movement disorders)
  2. Mesolimbic
    - VTA to nucleus accumbens
    - THERAPEUTIC SITE
  3. Mesocortical
    - VTA to frontal cortex
    - THERAPEUTIC SITE
  4. Hypothalamus
    - arcuate nucleus to medial eminence
    - tuberoinfundibular
    - prolactin release regulation
    - SIDE EFFECT -> ENDOCRINE DISORDERS
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9
Q

Which drug inhibits reuptake in NE neurons but not DA neurons?

A

Desipramine

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10
Q

MoA of typical antipsychotics

A

D2 receptor antagonists

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11
Q

Extrapyramidal DA side effects of typical antipsychotics

A
  1. Acute dystonia - Spasm of muscles of face, tongue, neck, and back
  2. Akathisia - Motor restlessness
  3. Parkinsonism - Rigidity, tremor, shuffling gait
  4. Tardive dyskinesia - Oral-facial involuntary movements, choreiform movement of extremities
    - late sign
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12
Q

Neuroleptic Malignant Syndrome

  • cause
  • symptoms
  • treatment
A

Reaction to antipsychotics (haldol hyperthermia)

Symptoms

  • Hyperthermia
  • Autonomic Instability
  • Muscle Rigidity

FEVER (from board)

  • fever
  • encephalopathy
  • vitals unstable
  • elevated enzymes
  • rigidity of muscles

Treatment
1. Withdraw typical antipsychotic
2. Cooling, hydration, supportive care
3. Dantrolene(muscle relaxant) for cooling
Bromocriptine (DA receptor agonist)

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13
Q

Endocrine DA side effects of typical antipsychotics

-hormonal change and effect

A
  1. Prolactin INCREASED
    Increased lactation, gynecomastia, etc.
    Inhibits ovulation, menses
    Decreased adrenal corticosteroid secretion
  2. Gonadotropins DECREASED
    Inhibits ovulation, menses
  3. Corticotropins DECREASED
    Decreased adrenal corticosteroid secretion
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14
Q

Adverse (non-DA) peripheral effects phenothiazines (e.g., chlorpromazine)

3 groups

A
  1. Anticholinergic activity
    - dry mouth
    - blurred vision
    - constipation
  2. alpha-adrenoceptor blockade
    - orthostatic hypoTN
    - inhibition of ejaculation
  3. Endocrine
    - appetite increase
    - weight gain
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15
Q

Huntington’s chorea can be txed with?

A

haloperidol - DA receptor antagonist

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16
Q

What is a major advantage in using atypical antipsychotics over typicals. Why do we get this advantage?

A

Much less EPS side effects (D2)

-not completely devoid but have a much higher therapeutic index than typicals

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17
Q

List 5 atypical antipsychotics (the ones in bold in the ppt)

A 
Aripiprazole
Olanzapine
Clozapine
Quetiapine 
Risperidone

It’s Atypical for Old Closets to Quietly Risper from A to Z

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18
Q

What’s a disadvantage of atypical antipsychotics? Give examples of this disadvantage

A

At normal doses, metabolic side effects are significant for atypical drugs

  • weight gain
  • metabolic problems
  • type 2 diabetes

Young and old must be given more attention

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19
Q

Serious side effect of Clozapine

  • percent of patients affected
  • etiology of the side effect?
A

Agranulocytosis (1-2% of patients; genetic). Testing Essential.

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20
Q

Which antipsychotic is a partial agonist at D2 DA receptors? Is it typical or atypical

A

Aripiprazole - atypical

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21
Q

Compare the efficacy between typical and atypical antipsychotics

A

Similar efficacy

~70% of patients

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22
Q

Acamprosate

  • MoA
  • use
A

Reduces the excitatory actions of glutamate at the NMDA receptor

-prevent severe w/drawal from alcohol

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23
Q

Disulfiram (antabuse)

  • MoA
  • side effect
A 
•	Inhibits aldehyde dehydrogenase (ALDH)
•	Use along with psychosocial support 
•	Compliance is an issue
•	Patient needs to monitored
o	Specially if they have other issues (e.g. heart)
•	Not used as much anymore
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24
Q

Naltrexone

  • MoA
  • side effects
  • check for what before starting?
A
  • Good evidence
  • Anti-relapse drug
  • Most common side effects = nausea and headache

• Nonselective opiate antagonist
o Reduces the reward component of drinking

• Run a basic liver panel before starting
o Hep B and C

  • Once a day pill
  • Use in combination w/ psychosocial treatments for best effect
25
Q

Acamprosate

  • MoA
  • used for
A

• Modulates the glutamate (indirectly blocks Glu effects on NMDA receptor)

• Diminishes post-acute withdrawal
o Weeks after people are off substances
o This time period is filled with discomfort for the patient

• Few side effects

26
Q

Sustained release Naltrexone

  • how is it administered?
  • benefits?
  • problems?
A
  • Given IM
  • New and expensive
  • Addresses compliance
  • Administered monthly
  • Vivitrol
  • Good for people with chaotic lives
27
Q

Most effective plan to treat alcohol dependence? Least effective?

A

Naltrexone in combination with medical mngt. found most effective.

Behavioral intervention alone, least effective.

28
Q

List 3 FDA approved pharmacological treatments for quitting nicotine

A

NRT
Bupropion SR
Varenicline tartate

29
Q

NRTs

  • types
  • effect on quit rate
  • precautions
A
  • gum, spray, inhalation
  • double the quit rate
  • precautions include
    1. pregnancy (class C)
    2. CV diseases
30
Q

Buproprion SR in Treating Nicotine Use Disorder

  • precaution (2)
  • contraindications (3)
  • side effects (2)
  • effect on quit rate
  • dosing
A

-precaution in pregnancy and CV diseases

-contraindicated in patients with
seizures
eating disorders
MAOI use w/in the past 14 days

-side effects
insomnia
dry mouth

-double quit rate

-dosing
• Begin 1-2 weeks before quit date
• Start at 150mg qAM for 3 days then ↑ to 150mg BID
• Maintain this dosage for 7-12 weeks following quit dat

31
Q

Varenicline tartate

  • MoA
  • used for
  • unique benefit
  • quit rate
A

MoA - partial agonist at the alpha4beta2 receptor

  • causes inhibition of GABA’s inhibition of DA
  • activates release of DA

Less cravings and w/drawal side effects

Smoking won’t lead to the same high
-leads to extinction

Triples quit rate short term
Long term quit rate less

32
Q

List to off label meds for nicotine use disorder

A

Nortriptyline and clonidine

33
Q

Nortriptyline

  • precautions
  • side effects
  • quit rate
A

-precautions in pregnancy and those w/ CV disease

side effects

  • sedation
  • dry mouth
  • urinary retention
  • risk of OD and cardiotoxicity

-doubles the quit rate

34
Q

Clonidine

  • precautions
  • risk of
  • side effects
  • quit rate
A
  • preg and CV disease
  • risk of rebound hypertension (taper dose)
  • side effects -> dry mouth, drowsiness, sedation and constipation
  • doubles quit rate
35
Q

5 C’s of addiction

A 
Chronic behavioral and mental disorder
Control of use impaired
Compulsive use
Continued use despite harm
Craving for the drug
36
Q

Type 1 vs type 2 substance craving behavior

  • trigger
  • NTs involved
A

Type 1

  • cue triggered
  • NT: glutamate

Type 2

  • stress triggered
  • CRF in amygdala
  • NE in brainstem
37
Q

Major reward site for alcohol

A

endorphin release by stimulation of mu opiate receptor

38
Q

How do stimulants (cocaine and amphetamines) work in the brain?

A

Enhance monoamine NT activity by inhibiting MAO reuptake in synapse

o DA – reward
o NE – physiological arousal
o 5-HT – elevated mood

39
Q

Mechanism for alcohol w/drawal - 3 things

A

Decrease in number of GABA receptors

Upregulation of NMDA receptors

  • leads to hyperexcitability
  • lower seizure threshold

Autonomic hyperactivity

  • inc noradrenergic activity in the LC
  • Benzos blunt this by stimulating GABA
40
Q

Opiate w/drawal mech and sxs

-how to reduce the sxs

A

o Internalization of mu opiate receptors

o Increased autonomic activity

o Hyperesthesia
-Increased perception of pain

o Dysphoria

o Admin opiate agonists mitigate sxs

o Clonidine diminishes noradrenergic effects for LC

  • Alpha blocker
  • Reduce the hyperactivity

o Nausea, vomiting, diarrhea
-Use antiemetic (e.g. Zofran)

41
Q

Stimulant w/drawal

A

Deplete DA from reward center (KNOW THIS)

• Decreased or lack of substance
– Severe dysphoria and drug craving
– Sleep disturbances and fatigue

42
Q

Topomax/topiramate for alcohol w/drawal

A

Anticonvulsants to regulate manic behavior

43
Q

Opioid agonists for opiate detox

A
  • methadone
  • buprenorphine
  • suboxone
44
Q

Issue w/ using naltrexone for opiate detox

A

-must be opiate free for 7 days

BLOCK ANALGESIA
-lot of pain

45
Q

Buprenorphine

  • MoA
  • why combined with naloxone (suboxone)
A

Partial mu agonist with HIGH AFFINITY

Precipitates w/dawal with recent opiate use

  • displace opioid from receptor
  • naloxone added to block action when used IV
46
Q

Methadone MoA

A
  • full mu agonist
  • long acting
  • low misuse potential
  • tx the w/drawal sxs from opiates
47
Q

Only activating antidepressant used to tx nicotine w/drawal

A

Bupropion

48
Q

Best evidence for NRT use

A

High dose replacement w/ transdermal + oral breakthrough craving

49
Q

chantix/varenicline

  • MoA
  • black box warning
A
  • partial agonist at nicotinic receptor

- increased suicide risk

50
Q

Arrange the therapies for depression based on most preferred to least

A

SSRI > SNRI > Atypicals > TCAs > MAOIs

51
Q

Side effects of lithium

-decrease in what makes Li+ more toxic?

A 
LMNOP
Lithium side effects:
-Movement (tremor)
-Nephrogenic diabetes insipidus
-HypOthyroidism 
-Pregnancy problems
52
Q

Carbamazepine

  • class
  • MoA
  • metabolism
  • side effects/contraindications
A
  • anticonvulsant
  • enhances inhibitory action of GABA by inhibiting VG Na channels
  • induced hepatic (CYP3A4) of itself
  • lots of drug-drug ix at the level of hepatic metabolism
  • serious skin rxns in HLA-58
  • teratogenic (category D)
53
Q

Valproic acid

  • class
  • MoA
  • drug-drug ix?
  • side effects/contraindications
A
  • anticonvulsant
  • inhibits Na and Ca channels -> activate GABA inhibitory effects
  • drug-drug interactions due to high serum protein binding
  • GI complaints; rare hepatic problems, tremor, sedation
  • Teratogenic (Pregnancy Category D)
54
Q

SSRIs - there are 4 (use mnemonic)

Flashbacks paralyze senior citizens

A

Fluoxetine, paroxetine, sertraline, citalopram

55
Q

Side effects of tricyclic antidepressants

A

Tri-C’s: Cardiotoxicity, convulsion, coma

56
Q

Major side effect of MAOI

A

hypertensive crisis especially when combined with 6mg tyramine

57
Q

most common side effects seen with SSRIs?

A

sexual dysfx and GI probs

58
Q

Name 2 SNRIs

A

Venlafaxine, duloxetine

59
Q

general Rule for naming TCAs

A

all TCAs end in -iptyline or -ipramine except doxepin and amoxapine

imipramine

BMB (15 decks)

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