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Pharmacology MD6 Flashcards

1
Q

Diphenhydramine

A
  • Opportunity for duplication of therapy and overdose (e.g. Benadryl and Sominex)
  • Ethanolamine, competitive 1st gen. H1 antagonist in GI, uterus, large blood vessels, bronchial muscle. Greater anticholinergic activity than other antihistamines.
  • CNS depression (sedative, OTC hypnotic), depress the cough center and dries the airways (antitussive), antiemetic/motion sickness, tx of allergic sx (edema, flare, pruritus)
  • FDA recommends no OTC cough or cold products (containing diphenhydramine among other ingredients) in children under 2 yrs.
  • Beers Criteria: Avoid in older adults d/t decr clearance ability-> incr anticholinergic effects, confusion, etc.
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2
Q

Anusol (hydrocortisone cream)

A
  • anti-inflammatory for hemorrhoids
  • MoA: binds glucocorticoid-R-> incr transcription of lipocortins (decr AA), decr cytokines
  • hemorrhoids are cushions in the anus that aid in bowel movements, they become pathological when the blood vessels w/in them become swollen and inflamed (often following straining during bowel movements).
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3
Q

Colchicine

A
  • tx of acute gout attack
  • oral, fecal & urinary excretion

*must be given w/in 24-48 h of onset

  • MoA: binds to tubulin inhibiting polymerization->
    1. inhibits mitotic spindle formation during mitosis in inflammatory cells
    2. prevents migration of granulocytes
    3. inhibitis synthesis & release leukotrienes
  • AE: GI upset, diarrhea, bone marrow suppression
  • CI: renal & hepatic impairment, concomitant use w/ CYP3A4 inhibitors
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4
Q

Allopurinol

A
  • oral or IV purine analog, 1st line prophylaxis in gout, uric acid stones, uric acid nephropathy
  • MoA: competitively inhibits xanthine oxidase preventing formation of uric acid, hypoxanthine & xanthine precursors are more water soluble and therefore less likely to precipitate
  • hypoxanthine and xanthine also cause negative feedback inhibition of purine synthesis
  • stimulates hypoxanthine & xanthine incorporation into DNA & RNA
  • -> decr serum uric acid
  • AE: hypersensitivity (skin rash in 3% of pts.)

*Drug-Drug Interactions: inhibits metabolism of 6-MP, azathioprine, theophylline

*Febuxostat: new XO inhibitor, same as allopurinol

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5
Q

Fentanyl

A

-opioid, fast & short-acting (anesthesia)

MoA: binds primarily mu-opioid receptors->

decr Ca entry-> decr presynaptic excitatory NT release

incr K efflux-> postsynaptic hyperpolarization-> decr response to excitatory NT

AE: resp. depression, dependence/abuse

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6
Q

Mannitol

A
  • tx of incr ICP/cerebral edema, IOP, (non tubular reabsorbed diuretic)
  • incr osmolality of blood-> pulls water from CSF-> decr ICP

CI: CHF, pulmonary edema (incr volume in blood), active intracranial bleed

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7
Q

Pancuronium, Vecuronium

A

non-depol muscle relaxant (ET intubation, mechanical vent.), longer-acting

MoA: competitive antagonist @ nicotinic ACh receptors on skeletal muscle, can be overcome by incr ACh (cholinesterase inhibitors)

AE: weak antimuscarinic

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8
Q

Midazolam, Diazepam

A

Midazolam: short-acting benzo for sedation/anxiolytic/amnesic

Diazepam: long-acting for muscle spasms/anxiolytic/ethanol withdrawal/antiepileptic (muscle relaxant MoA: no direct NMJ/muscle action)

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9
Q

Methocarbamol

A

MoA: central CNS depression-> decr muscle spasms (no direct NMJ/muscle action)

AE: sedation

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10
Q

Cyclobenzaprine

A

5HT2 antagonism (similar to TCAs)-> decr serotonergic stimulation of motor activity (no direct NMJ/muscle action)

AE: CNS depression, anticholinergic (TCA-like)

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11
Q

Methotrexate

A

-inflammatory arthritis, neoplasms

MoA:

  1. inhibit DHFR-> decr thymine production-> decr DNA synthesis & cytotoxicity in high metabolic rate cells (neoplasms)
  2. inhibit AICAR transformylase-> incr adenosine-> feedback inhibit lymphocytes (which lack purine salvage pathway)

AE: bone marrow suppression, teratogenic

Interactions w/: gold (pulmonary toxicitiy), azathioprine (hepatotoxicity)

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12
Q

Azathioprine

A

converted to 6-MP, inhibits IMP dehydrogenase and PRPP-> decr purine synthesis (mainly affecting lymphocytes, which lack salvage pathway)

AE: immunosuppression (leuko, thrombocytopenia, anemia) incr risk of malignancy (lymphoma)

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13
Q

Calcipotriene

A

Vit D3 analog-> binds Vit D receptors on skin-> inhibits cell proliferation-> tx of psoriasis (hyperproliferation of keratinocytes)

AE: hyperCa

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14
Q

Gentamicin

A

aminoglycoside for Gram - anaerobes

MoA: O2-dependent transport to enter bacterium-> binds 30S ribosomal subunit-> premature termination, mistranslation, and/or prevention of initiation of protein translation

AE: oto & nephrotoxicity

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15
Q

Mitoxantrone

A

DNA intercalation-> inter/intrastrand cross-links and breakage

-specifically affects lymphocytes in MS

tx of leukemias, MS (only if other tx options fail)

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16
Q

IFN-B1a/b

A

tx of MS (dz modifying, 1st line)

MoA: inhibition of T lymphocytes via (decr proinflammatory cytokines, incr T regs, decr migration)

slow progression and decr atk rate

AE: flulike sx

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17
Q

Glatiramer acetate

A

1st line tx for MS

MoA: compete w/ MBP for binding to MHC?

slow progression, decr atk rate

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18
Q

Natalizumab

A

monoclonal Ig vs a4-integrin (2nd line for MS)

MoA: prevents adhesion and CNS migration of lymphocytes

AE: incr risk of PML (JC virus infxn)

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19
Q

TNF inhibitors

A

Etanercept (decoy receptor for TNFa), Adalimumab (monoclonal antibody vs TNFa)

-dz modifying agents for RA

*important to check PPD prior to initiation, since TNF modulates granuloma formation (inhibition of TNF may allow reactivation of TB infxn)

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20
Q

Lupus Tx

A

Mild dz (no vital organ involvement):

  • NSAIDs
  • Hydroxychloroquine: antimalarial, antiinflam (?MoA)

AE: ocular toxicitiy

Severe dz (vital organ involvement)

  • long-term corticosteroid use
  • immunosuppressants:
  1. Cyclophosphamide (alkylating agent), AE: hemorrhagic cystitis, marrow suppression, CI in pregnancy
  2. Chlorambucil (similar to cyclophosphamide, usually for CLL)
  3. Mycophenolate mofetil (inhibit IMP dehydrogenase-> decr guanosine synthesis)
  4. Azathioprine (purine analog, decr purine synthesis, not as effective): can give in pregnancy

Antiphospholipid Antibody Syndrome:

lifetime coagulation (warfarin or heparin + aspirin during pregnancy)

Skin manifestations:

topical corticosteroids (hydrocortisone), sunblock

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21
Q

Dicumarol

A

Vit K inhibitor like Warfarin, but more drug interactions and less predictable effects

  • no longer used in U.S.
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22
Q

Calcium EDTA

A

chelating agent (lead replaces Ca2+) used to bind lead during lead poisoning, incr solubility, for renal excretion

23
Q

Allopurinol

A

tx of hyperuricemia

MoA: inhibits xanthine oxidase-> decr formation of xanthine from hypoxanthine & guanine, and uric acid from xanthine

  • 1st line for lowering of uric acid levels (chronic tx),
  • AE: decr metabolism of azathioprine & 6-MP via xanthine oxidase

Febuxostat:

  • newer version of allopurinol, same MoA
24
Q

Colchicine

A

tx of acute gout attacks

MoA: inhibit tubulin polymerization-> decr mitotic spindle formation-> decr inflammatory cell migration and granulation

*used in acute gout attacks along with NSAIDs, and sometimes glucocorticoids

25
Other Gout Drugs
_Probenecid_ * decr PCT reabsorption of uric acid * AE: may form uric acid urolithiasis
26
Ethosuximide
Tx of absence sz MoA: inhibits thalamic T-type Ca channels AE: Stevens-Johnson
27
Benzodiazepines for Status Epilepticus (Diazepam: long-acting)
MoA: bind BNZ2 receptors increasing freq. of GABAa-mediated Cl- channel opening-\> hyperpol. * acute tx of status epilepticus
28
Phenytoin
tx of GTC sz, prophylaxis of status epilepticus MoA: inhibit Na channel activation AE: P-450 inducer, Stevens-Johnson, megaloblastic anemia, SLE, fetal hydantoin syndrome (short nails, fingers) \*zero-order kinetics
29
Carbamazepine
tx of GTC sz, partial sz, trigeminal neuralgia MoA: inhibit Na channel activation AE: P-450 inducer, Stevens-Johnson, aplastic anemia/agranulocytosis, SIADH
30
Valproic Acid
tx of GTC sz, 2ndary for all other sz MoA: inhibit Na channel activation, inhibit GABA transaminase (incr GABA) AE: hepatotox, spina bifida, thrombocytopenia
31
Phenobarbital
barbiturate indicated for tx of neonatal sz MoA: prolongs GABA-mediated opening of Cl- channels-\> hyperpol. AE: sedation, resp depression, abuse \> benzos, P-450 inducer
32
Succinylcholine
depol. muscle relaxant, short-acting for induction of paralysis during sx MoA: sustained binding to nicotinic ACh-R leading to prolonged depol.-\> ACh-Rs remain in inactive state, cannot be broken down by AChE or overcome by ACh AE: black box warning of rhabdomyolysis in pediatrics-\> hyperK & cardiac arrhythmias, hyperthermia
33
Pyridostigmine, Neostigmine
pyridostigmine is _1st line tx of MG_, prophylaxis for nerve gas exposure * longer-acting & decr muscarinic AEs vs. neostigmine MoA: competes (reversible) w/ ACh for binding of AChE-\> decr ACh degradation-\> incr ACh in NMJ \*Edrophonium is old cholinesterase inhibitor used to test for MG, however, no longer used as Dx. Not used as Tx d/t very short duration of action AE: cholinergic stimulation (DUMBBELSS)
34
Atropine
antimuscarinic used in AChEI poisoning (organophosphates) MoA: competitive inhibitor of ACh @ muscarinic receptors (no action @ nicotinic) AE: anticholinergic effects
35
Organophosphates
insecticides, herbicides, nerve gases MoA: phosphorylate AChE-\> inactivation & incr of ACh-\> overstimulation of muscle-\> muscle paralysis (respiratory failure if occurs in respiratory muscles), also respiratory center depression (CNS nicotinic receptors)
36
Levo-dopa + Carbidopa
* 1st line tx in PD * L-dopa is dopamine precursor that can cross BBB, carbidopa prevents peripheral degradation by dopa decarboxylase * decr peripheral dopamine AEs (n/v, arrythmia (incr catecholamines) * AE: "on-off" phenomenon (incr over time): dyskinesia \> therapeutic levels, bradykinesia \< therapeutic levels * CI for long-term use d/t incr neurodegeneration and in psychotic pts (exacerbate) * decr response to L-dopa = not PD
37
Dopamine agonists
* Bromocriptine (non-ergot): not used d/t cardiac valvular AEs * Non-ergots (Pramipexole (D2/indirect primarily) and Ropinirole) * not as effective vs L-dopa, but longer lasting and less on-off phenomenon
38
Amantadine
NMDA-R antagonist, incr dopamine release
39
Selegiline
* MAO inhibitor, type B (primarily dopamine) * prevents dopamine breakdown by MAO in the CNS * ?Dz modifying effects (use in younger pts) * decr off time vs L-dopa * AE: @ high doses, inhibits MAO-A-\> incr catecholamines-\> HTN
40
Benztropine
antimuscarinic, CNS * primarily for tremor use d/t MoA of decr ACh * give w/ haloperidol to prevent EPS * CI: elderly (memory problems)
41
COMT inhibitors
Entacapone (peripheral only), Tolcapone (both) * prevent dopamine breakdown by COMT in GI & liver * less on-off
42
Methylphenidate (Ritalin)
CNS stimulant, 1st line tx of ADHD MoA: blocks dopamine & norepinephrine transporters preventing reuptake-\> incr DA & NE Incr attention span, alertness, ability to complete tasks, euphoria Decr fatigue, distractability, impulsivity AE: insomnia, anorexia, wt loss, potential for abuse (also non-ADHD persons using) \*ineffective in up to 1/3 of ADHD \*less potential for abuse than other stimulants (e.g. cocaine)
43
Amphetamines (Adderall, dextroamphetamine)
1st line tx of ADHD MoA: incr release of NE (lower doses) and DA (higher doses) into synaptic cleft Incr attention span, alertness, ability to complete tasks, euphoria Decr fatigue, distractability, impulsivity AE: insomnia, anorexia, wt loss, potential for abuse (also non-ADHD persons using) \*ineffective in up to 1/3 of ADHD
44
Atomoxetine
SNRI, 2nd line for ADHD MoA: prevent NE reuptake less abuse potential vs stimulants
45
Donepezil, Rivastigmine, Galantamine
AChE inhibitors-\> incr ACh in synapse-\> improve cognition, delay decline 1st line tx in AD
46
Memantine
NMDA-R antagonist-\> prevents glutamate-mediated excitotoxicity in neurons (Ca2+) \*low affinity binding still allows physiologic glutamate mediated learning to occur used in conjunction w/ AChEIs to improve cognition, delay decline in AD (moderate-severe AD)
47
Atypical Antipsychotics
MoA: * 5-HT2A blockade-\> decr inhibition of DA in mesocortical-\> **tx of - sx** * weaker blockade of D2-\> tx + sx (mesolimbic) w/ less EPS \*usually 1st line tx of schizophrenia AE: all antipsychotics may cause QT prolongation & black box warning of incr mortality in elderly w/ dementia, less anticholinergic/histamine/adrenergic AEs vs typicals _Clozapine:_ used in refractory pts d/t AE of agranulocytosis _Olanzapine_ AE: weight gain, diabetogenic _Risperidone_ AE: hyperPRL _Aripiprazole_ partial DA agonist/antagonist _Ziprasidone_ incr risk of QT prolongation
48
Typical Antipsychotics (Neuroleptics)
MoA: blockade of D2 receptors-\> tx of **+ sx** (mesolimbic) AE: EPS, anticholinergic/histamine/adrenergic, possible worsening of - sx **EPS: dystonia (h), akathisia/restlessness (d), parkinsonisms (w)** **Tardive dyskinesia** (m-y): antipsychotic use-\> D2 hypersensitivity/upregulation-\> irreversible choreoathetosis & oral-facial dystonias, worse w/ anticholinergics **Neuroleptic Malignant Syndrome (NMS):** ***F***ever (hyperthermia) ***E***ncephalopathy ***V***ital signs (autonomic) ***E***nzymes (CK, myoglobinuria) ***R***igidity * tx w/ dopamine agonist (Bromocriptine), muscle relaxant (Dantrolene, SR Ca block) High Potency: _Haloperidol_, _Fluphenazine_, _Trifluoperazine_ * incr EPS, less anticholinergic/histamine/adrenergic Low Potency: * incr anticholinergic/histamine/adrenergic _Chlorpromazine_ **C**orneal deposits _Thioridazine_ re**T**inal deposits \*all antipsychotics incr risk of QT prolongation, black box warning of incr mortality in elderly w/ dementia
49
Lithium
1st line for mania, especially effective in cyclothymic disorder MoA: ? PIP inhibition AE: low therapeutic index Movement (tremor) Nephrogenic diabetes insipidus hypOthyroidism Pregnancy (Ebstein anomaly)
50
Selective Serotonin Reuptake Inhibitors (SSRIs)
* 1st line depression (less AE vs TCAs, MAOIs), everything else except mania and psychosis MoA: prevent 5-HT reuptake-\> incr 5-HT-\> bind autoregulatory 5-HT1 receptors-\> downregulation over time (takes 4-8 wks)-\> incr serotonergic activity Flashbacks Paralyze Flatulent Senior Citizens **F**luvoxamine: OCD tx **F**luoxetine: indicated in 8+ y/o children **P**aroxetine **S**ertraline **C**italopram AE: SIADH, delayed ejac., insomnia, nausea * Serotonin Syndrome (+ TCAs, MAOIs, meperidine, dextromethorphan)-\> hyperthermia, confusion, sz, **myoclonus**, **flushing, diarrhea** * *Tx with cyproheptadine*
51
Tricyclic Antidepressants (TCAs)
MoA: inhibit reuptake of NE & 5-HT \*use nortryptiline in elderly (decr sedation) **CANDIDA** **C**lomipramine **A**mitryptiline **N**ortryptiline **D**esipramine **I**mipramine **D**oxepin **A**moxapine AE: HAM: antimuscarinic (amitryptiline & imipramine), adrenergic blockade 3 Cs: coma, convulsions, cardiotoxicity
52
Monoamine Oxidase Inhibitors (MAOIs)
tx of atypical depression MoA: prevent metabolism of 5-HT, NE, tyramine (A), dopamine (B) in nerve endings-\> incr release Nonselective (tranylcypromine, phenelzine) Selective: Selegiline (B): dopamine only AE: Hypertensive crisis when eating wine & cheese (incr tyramine-\> incr catecholamines) Hypotension over time?
53
Selective Norepinephrine Reuptake Inhibitors (SNRIs)
MoA: prevent reuptake of 5-HT (low doses), NE (incr doses) _Venlafaxine_: TAP (trauma/PTSD, anxiety, panic) _Duloxetine_ AE: less HAM, incr CNS stimulant
54
Benzodiazepines
Diazepam, Chlordiazepoxide, Flurazepam (long-acting) = less sedation Lorazepam (intermediate): tx of acute anxiety Alprazolam (intermediate, acute onset): panic, phobias AE: sedation, resp depr, dependence, enhanced etoh \*Flumazenil for overdose

Pharmacology (7 decks)

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