A: 29-33 Flashcards
(56 cards)
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
2
Q
Maprotiline MOA
A
- tetracyclic antidepresant
NET>>SERT
3
Q
Maprotiline indication
A
- tetracyclic antidepressant : inhibit NET
- Major depression
- Sedation
overdoses of maprolitine can cause seizures (it lowers convulsive threshold)
4
Q
Maprotiline SE
A
- seizures
- cardiotoxic
in case of overdose
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
6
Q
Tricyclic MOA
A
Like SNRI
Inhibit NET and SERT
7
Q
Tricyclic SE are due to
A
Muscarinic, a1, H1 blockade (sedation and weight gain)
8
Q
TCA indication
A
- Major depression
- chronic pain
- OCD ( clomipramine)
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
10
Q
SSRI’s indication
A
Major depressive disorder
Anxiety
OCD
PMDD (Premenstrual Dysphoric Disorder )
PTSD
Bolemia
11
Q
SSRI’s metabolism
A
Inhibitors of CYP450
half life +15 hrs
- cyp2d6 , CYP3A4 inhibition ( Fluxetine, paroxetine)
- CYP1A2 : fluvoxamine
12
Q
SSRI SE
A
sexual dysfunction
agitation
insomnia
headache
nausea
anxiety
citalopram - QT prolongation
13
Q
SNRTI’s
A
בוא נלך לאכול בוואן לאפה ונשתה רבוקס דלוקס
Venlafexine
Reboxetine(Only NET)
Duloxetine
14
Q
SNRI indication
A
- Major depression
- chronic pain
- fibromyalgia
- menopausal symptoms
15
Q
SNRI SE
A
- Anticholinergic
- sedation
- hypertension (Venlafaxine)
16
Q
NE-R antag. for antidepression
A
Mitrazapine is an a2 antagonist (block presynaptic a2 r)
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
- hypnosis (trazodone)
- short T1/2
-
Trazodone
18
Q
Trazodone indication
A
- 5-HT2 antagonist
- Major depression
- hypnosis
19
Q
Trazodone SE
A
- 5-HT2 blocker
- sedation
- modest alpha and H1 blockade
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
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
22
Q
MAO-I
drugs and mechanism
A
- Moclobemide (MAO-A selective inhibitor) - antidepressant
- Selegilime (more active as MAO-B inhibitor)- anti-parkinsons
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
Mirtazapine mechanism, indication
* a-2 selective blocker \> increased amine release
* 5-HT2, 5-HT3 inhibitor
* H1-r inhibition
* major depressive disorders
* sedation
SE: weight gain , sedation
26
Lithium indication
* Bipolar affective disorder
* prevents modd swings (prophylaxis)
27
lithium mechanism of action
* 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
Lithium SE
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
Valproate MOA
* 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
Valproate indication
* Generalized tonic-clonic
* focal
* myoclonic seizure
* Bipolar disorder: competes with lithium as first choice in bipolar (acute phase)
Valproate phase 2 (conjugation)
31
valproate SE
* hepatic dysfunction,
* weight gain,
* and inhibition of drug metabolism (valproic acid)
* teratogenic
* pancreatitis
* GI distress
* thrombocytopenia - monitor PLT
32
Carbamazapine MOA
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
Carbamazapine indication
* Generalized tonic-clonic
* focal seizures
* Bipolar disorder (acute and prophylaxis)
* trigeminal neuralgia (1st line)
oral, P450 metabolism
Carbamazepine forms active metabolite (phase I);
34
Carbamazapine SE
* **Hematotoxicity** and
* induction of drug metabolism (carbamazepine)
* CNS dep (dose-dep)
* diplopia
* SJS
* SIADH
* Aplastic anemia
* teratogenic
35
Anti epileptic which are NOT broad spectrum
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
T1/2 of SSRI vs SNRI
* SSRI (citalopram, fluoxetine, sertraline) : 15+ hrs
* SNRI (Venlafaxine, desvenlafaxine, duloxetine) : 10+ hrs
37
Tonic-clonic seizure (grand mal) characteristerics and drugs which can be used
* 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
partial seizure /focal
characteristerics and drugs which can be used
* 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
Generalized absence seizure "petit mal"
characteristerics and drugs which can be used
* 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
myoclonic seizure characteristics and drugs
* Consist of sudden, brief movement which are not ass w/ any disturbance of conciousness
* Clonazepam
* Lamotrigine
* valproic acid
41
status epilepticus characteristics and drugs
* 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
A32 antiepileptics used in partial seizures and generalised tonic-myoclonic seizures
EXCEPT broad spectrum agents
* **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
Broad spectrum antiepileptics
* **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
Levetiracetam-
moa
* Binds synaptic protein SV2A ,
* modifies GABA
* modifies Glutamate release. לב לתירצה סתם
45
levetiracetam IND
IND:
* Generalised tonic-clonic
* focal seizure
46
levetiracetam SE
* dizzy,
* nervous,
* depression,
* seizure
47
Ethusoximide-
MOA, indication
* inhibits Thalamic Ca2+ Ch. (T-type) Alot of Ethous to work on the Thelamic
* IND: absence seizure
* long T1/2
48
SE ethusoximide
* GI distress.
* dizzy,
* headache
49
Lamotrigine-
MOA
* Inhibits Na axonal channels.
* Inhibits Ca +2 channel
* decreases neuronal glutamate release למה לא?TRIGGED?
50
Lamotrigine IND
* IND:
* generalised tonic-clonic
* focal seizure
* myoclonic
* absence seizure
51
LAMOTRIGINE SE
SE:
* dizzy,
* diplopia,
* headache,
* rash
52
Valproate-
MOA
inhibits Thalamic Ca2+ Ch (blocks high freq firing)
53
Valproate ind
IND:
* generalised tonic-clonic
* focal
* myoclonic
54
valproate SE
* nausea ,
* alopecia,
* weight gain,
* teratogenic
55
Diazepam-
moa, ind
enhance GABA-A
IND: status epilepticus
56
Clonazepam-
moa, ind, SE
* enhance GABA-A
* IND:
* Absence seizure
* myoclonic seizure
* infantile spasms
SE: sedation
