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Pharmacology FINAL (2nd sem) > A: 29-33 > Flashcards

A: 29-33 Flashcards

1
Q

Tricyclic
Tetracyclic
Unicyclic
MAO-inhib

A
  • Tricyclic-
    • Amitriptyline
    • Clomipramine. Ami tripped the line, כלום לא ישנה את הפרייד שלי
    • Imipramine
  • Tetracyclic-
    • Maprotiline. מה פרו? טיל!
  • Unicyclic- Bupropion. Bu!prop!yon!
  • MAO-inhib-
    • Moclobemide MAoclobemide
  • 5HT-2 inhibitor
    • Trazodone

AC-M-B-M-T
CAM Be with Me
Trazodone is a 5HT inhibitor

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2
Q

Maprotiline MOA

A
  • tetracyclic antidepresant

NET>>SERT

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3
Q

Maprotiline indication

A
  • tetracyclic antidepressant : inhibit NET
  1. Major depression
  2. Sedation

overdoses of maprolitine can cause seizures (it lowers convulsive threshold)

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4
Q

Maprotiline SE

A
  • seizures
  • cardiotoxic

in case of overdose

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5
Q

Bupropion, structure , mechanism , indication

A
  • Heterocyclic antidepressant
  • mechanism is unknown—the drug has NO effect on either 5-HT or NE receptors or on amine transporters
    1. Major depresion
    2. smoking cessation
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6
Q

Tricyclic MOA

A

Like SNRI
Inhibit NET and SERT

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7
Q

Tricyclic SE are due to

A

Muscarinic, a1, H1 blockade (sedation and weight gain)

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8
Q

TCA indication

A
  • Major depression
  • chronic pain
  • OCD ( clomipramine)
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9
Q

SSRI’s

A

Work in the brain so CSF!
Sir. Tralin! the Chita-lo-pram has Flu so EXIT!

Sertraline
Citalopram
Fluoxetine

T1/2 +15 hrs

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10
Q

SSRI’s indication

A

Major depressive disorder
Anxiety
OCD

PMDD (Premenstrual Dysphoric Disorder )
PTSD
Bolemia

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11
Q

SSRI’s metabolism

A

Inhibitors of CYP450

half life +15 hrs

  • cyp2d6 , CYP3A4 inhibition ( Fluxetine, paroxetine)
  • CYP1A2 : fluvoxamine
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12
Q

SSRI SE

A

sexual dysfunction

agitation

insomnia

headache

nausea

anxiety

citalopram - QT prolongation

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13
Q

SNRTI’s

A

בוא נלך לאכול בוואן לאפה ונשתה רבוקס דלוקס

Venlafexine
Reboxetine(Only NET)
Duloxetine

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14
Q

SNRI indication

A
  • Major depression
  • chronic pain
  • fibromyalgia
  • menopausal symptoms
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15
Q

SNRI SE

A
  • Anticholinergic
  • sedation
  • hypertension (Venlafaxine)
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16
Q

NE-R antag. for antidepression

A

Mitrazapine is an a2 antagonist (block presynaptic a2 r)

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17
Q

5-HT antagonist for antidepression

A

Agomelatine is also agonist at MT1/2 r in suprachiasmatic nucleus + 5-HT 2/3 antagonist

  • major depressive disorder
  • 5-HT2 antagonist
    • Trazodone
      • ​ind: 1. Major depression
        1. hypnosis (trazodone)
      • short T1/2
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18
Q

Trazodone indication

A
  • 5-HT2 antagonist
  • Major depression
  • hypnosis
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19
Q

Trazodone SE

A
  • 5-HT2 blocker
  • sedation
  • modest alpha and H1 blockade
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20
Q

agomelatine

A

Agomelatine is

  • agonist at MT1/2 r in suprachiasmatic nucleus
  • 5-HT 2/3 antagonist

major depressive disorder

SE: weight gain

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21
Q

MAO-I indication and SE

A
  • Major depression unresponsive to other drugs
  • SE:
    • Hypotension
    • insomnia
    • Serotonin syndrome if combined with SSRI
    • Hypetension with tyramine and sympathomimetics
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22
Q

MAO-I

drugs and mechanism

A
  • Moclobemide (MAO-A selective inhibitor) - antidepressant
  • Selegilime (more active as MAO-B inhibitor)- anti-parkinsons
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23
Q

MAO-I drug interactions

A

Hypertension with tyramine and sympathomimmetics

serotonin syndrome if combined with SSRI

very long T1/2

24
Q

MAO A metabolises?

MAO-B metabolises?

A
  • MAO-A
    • NE
    • 5-HT
    • Tyramine
  • MAO-B
    • Dopamine
25
Q

Mirtazapine mechanism, indication

A
  • a-2 selective blocker > increased amine release
  • 5-HT2, 5-HT3 inhibitor
  • H1-r inhibition
  • major depressive disorders
  • sedation

SE: weight gain , sedation

26
Q

Lithium indication

A
  • Bipolar affective disorder
  • prevents modd swings (prophylaxis)
27
Q

lithium mechanism of action

A
  • Uncertain, it inhibit several enzymes involved in recycling of neuronal membrane phosphoinositides.;
  • supresses IP3 , DAG signalling (interfere with Gq)
  • inhibits GSK-3
  • NO action on ANS receptors or CNS receptors
  • NO sedation

renal elimination

T1/2 = 20hrs

28
Q

Lithium SE

A

Reversible hypothyroidism
DI (bcs Li+ antag ADH-R) - renal dysfunction
Tremor
Ataxia
Nephrogenic DI

Edema

CI: pregnancy (neural tube defect)

  • Narrow therapeutic window - monitor blood levels
  • clearance is decreased by
    • thiazides
    • NSAIDS
29
Q

Valproate MOA

A
  • Inhibits of voltage-gated Na channels in neuronal membranes
  • Inhibits T-type Ca channel (in thalamic neuron)
  • increased brain levels of GABA by Inhibiting GABA-aminotransaminase which normally terminates GABA action. ( for the Tx. of the manic phase)
  • Increases neuronal K+ permeability (neuronal membrane hyperpolarization.

Blocks high-frequency firing

30
Q

Valproate indication

A
  • Generalized tonic-clonic
  • focal
  • myoclonic seizure
  • Bipolar disorder: competes with lithium as first choice in bipolar (acute phase)

Valproate phase 2 (conjugation)

31
Q

valproate SE

A
  • hepatic dysfunction,
  • weight gain,
  • and inhibition of drug metabolism (valproic acid)
  • teratogenic
  • pancreatitis
  • GI distress
  • thrombocytopenia - monitor PLT
32
Q

Carbamazapine MOA

A

Extends the inactivated phase of Na+ Ch. on the axon so no AP

  • Blocks axonal VG- Na channel
  • decreases glutamate release
  • prevents seizure propagation, but NOT initiation
33
Q

Carbamazapine indication

A
  • Generalized tonic-clonic
  • focal seizures
  • Bipolar disorder (acute and prophylaxis)
  • trigeminal neuralgia (1st line)

oral, P450 metabolism

Carbamazepine forms active metabolite (phase I);

34
Q

Carbamazapine SE

A
  • Hematotoxicity and
  • induction of drug metabolism (carbamazepine)
  • CNS dep (dose-dep)
  • diplopia
  • SJS
  • SIADH
  • Aplastic anemia
  • teratogenic
35
Q

Anti epileptic which are NOT broad spectrum

A

Phenytoin- Inhib. of axonal NaCh
Carbamazapine- -“-
Vigabatrin- Inhibits GABA metab.
Phenobarbital- GABA NaCh open longer

Very Privet Cards Play
Privet bcs it is narrow spectrum

36
Q

T1/2 of SSRI vs SNRI

A
  • SSRI (citalopram, fluoxetine, sertraline) : 15+ hrs
  • SNRI (Venlafaxine, desvenlafaxine, duloxetine) : 10+ hrs
37
Q

Tonic-clonic seizure (grand mal) characteristerics and drugs which can be used

A
  • Bilateral symmetric convulsive movements of all limbs with impairment of conciousness
    • Tonic phase (<1min) : loss of consciousness , muscle stiffening
    • Clonic phase ( 2-3 min) : jerking of body muscles
  • Valproic acid
  • phenytoin
  • Carbamazepine
  • Phenobarbital
  • Lamotrigine
  • Leve-tiracetam
38
Q

partial seizure /focal

characteristerics and drugs which can be used

A
  • Involves focal cortical region at onset
    • simple partial seizure > no loss of conciousness
    • complex partial seizure > loss of conviousness/impaired awareness
  • Phenytoin
  • Carbamazepine
  • Gabapentin
  • pregabalin
  • vigabatrin
  • Valproate
  • lamotrigine
  • levetiracetam
39
Q

Generalized absence seizure “petit mal”

characteristerics and drugs which can be used

A
  • Impaired concioussness
  • starts with unresponsiveness to external verbal stimuli ( sometimes with eye blinking and head nodding)
  • Ethosuximide (minimal sedation; preffered)
  • valproate (minimal sedation; preffered)
  • clonazepam
  • lamotrigine
  • levetiracetam
40
Q

myoclonic seizure characteristics and drugs

A
  • Consist of sudden, brief movement which are not ass w/ any disturbance of conciousness
  • Clonazepam
  • Lamotrigine
  • valproic acid
41
Q

status epilepticus characteristics and drugs

A
  • continuous seizure lasting more than 5 mins OR >2 seizures without full recovery of conciousness between any of them
  • life-threatening, medical emergency
  • Lorazepam
  • Diazepam
  • Phenytoin (may cause cardiotoxicity due to solvent propylene glycol) , fosphenytoin (water-soluble)
  • Phenobarbital
  • In severe cases which DONT respond to anti-convulsant , general anesthesia may be used
42
Q

A32 antiepileptics used in partial seizures and generalised tonic-myoclonic seizures

EXCEPT broad spectrum agents

A
  • Phenobarbital
    • Enhances GABA-A r responses
    • ind:
      • generalised tonic-clonic seizure
      • focal seizures
    • SE: sedation, ataxia
  • Phenytoin
    • blocks VG Na ch
    • IND:
      • generalised tonic-clonic
      • focal seizures
    • SE: ataxia, diplopia, gingival hyperplasia, hisutism, neuropathy
  • carbamazepine
    • blocks VG Na+ ch
    • decreases Glutamate release
    • IND:
      • generalised tonic-clonic
      • focal seizures
    • SE: Ataxia, diplopia, headache, nausea
  • vigabatrine (GABA derivative)
    • inhibit GABA-transaminase ( inhibited by valproate too)
      • IND:
        • focal seizures ONLY
      • renal elimination
      • SE: drowsy, dizzy, psychosis, ocular effect
43
Q

Broad spectrum antiepileptics

A
  • Ethusoximide-
    • inhibits Thalamic Ca2+ Ch. (T-type) Alot of Ethous to work on the Thelamic
    • IND:
      • absence seizure
    • long T1/2
    • SE: GI distress. dizzy, headache
  • Lamotrigine-
    • Inhibits Na axonal channels.
    • Inhibits Ca +2 channel
    • decreases neuronal glutamate release למה לא?TRIGGED?
    • IND:
      • generalised tonic-clonic
      • focal seizure
      • myoclonic
      • absence seizure
    • SE: dizzy, diplopia, headache, rash
  • Levetiracetam-
    • Binds synaptic protein SV2A , modifies GABA and Glutamate release. לב לתירצה סתם
    • IND:
      • Generalised tonic-clonic
      • focal seizure
    • SE: dizzy, nervous, depression, seizure
  • Valproate-
    • inhibits Thalamic Ca2+ Ch (blocks high freq firing)
    • IND:
      • generalised tonic-clonic
      • focal
      • myoclonic
    • SE: nausea , alopecia, weight gain, teratogenic
  • Clonazepam-
    • enhance GABA-A
    • IND:
      • Absence seizure
      • myoclonic seizure
      • infantile spasms
    • SE: sedation
  • Diazepam-
    • enhance GABA-A
    • IND: status epilepticus

VECLLD

44
Q

Levetiracetam-

moa

A
  • Binds synaptic protein SV2A ,
  • modifies GABA
  • modifies Glutamate release. לב לתירצה סתם
45
Q

levetiracetam IND

A

IND:

  • Generalised tonic-clonic
  • focal seizure
46
Q

levetiracetam SE

A
  • dizzy,
  • nervous,
  • depression,
  • seizure
47
Q

Ethusoximide-

MOA, indication

A
  • inhibits Thalamic Ca2+ Ch. (T-type) Alot of Ethous to work on the Thelamic
  • IND: absence seizure
  • long T1/2
48
Q

SE ethusoximide

A
  • GI distress.
  • dizzy,
  • headache
49
Q

Lamotrigine-

MOA

A
  • Inhibits Na axonal channels.
  • Inhibits Ca +2 channel
  • decreases neuronal glutamate release למה לא?TRIGGED?
50
Q

Lamotrigine IND

A
  • IND:
    • generalised tonic-clonic
    • focal seizure
    • myoclonic
    • absence seizure
51
Q

LAMOTRIGINE SE

A

SE:

  • dizzy,
  • diplopia,
  • headache,
  • rash
52
Q

Valproate-

MOA

A

inhibits Thalamic Ca2+ Ch (blocks high freq firing)

53
Q

Valproate ind

A

IND:

  • generalised tonic-clonic
  • focal
  • myoclonic
54
Q

valproate SE

A
  • nausea ,
  • alopecia,
  • weight gain,
  • teratogenic
55
Q

Diazepam-

moa, ind

A

enhance GABA-A

IND: status epilepticus

56
Q

Clonazepam-

moa, ind, SE

A
  • enhance GABA-A
  • IND:
    • Absence seizure
    • myoclonic seizure
    • infantile spasms

SE: sedation

Pharmacology FINAL (2nd sem) (37 decks)

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