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					                       2008 Pharm Exam 1

                   Seizures/Anticonvulsants
Seizures = hyperactivity of NMDA receptor (glutamate)
Drugs = encourage inactivatins of Na/Ca channels

                           Na channel Blockers
Phenyltoin:
Use= chronic tonic seizure
Contraindication: myoclonic seizure
Mechanism: reduces potentiation from seizure focus (blocks Na channel),
oral absorbtion
* can‟t be injected, (other form „fosphenytoin‟ injected instead)
* gingival hyperplasia

Carbamazepine/oxcarbazepine:
Use: Tonic clonic, neuralgia
Contra: myoclonic
Mech: Inactivates voltage gated Na, oral absorption



                         Na/Ca channel Blockers
Lamotrigine:
Use: complex, myoclonic
Mech: more potent Na blocker than „phenyltoin‟, also ca blocker

Leviteracetam:
Use: complex partial seizure and tonic clonic
Mech: na/ca vesicles

Valproic acid/valproate:
Use: Tonic clonic and Epson(mild) seizures, neuralgia
Contra: hepatic disease
Mech: inactivates Na/ca(t-type) channels
                             Ca channel Blockers
Ethosuximide:
Use: Myoclonic
Contra: tonic clonic

Zonisamide:
Use: myoclonic seizures
Mech: blocks Ca channels

                         Ca channel blocker (PAIN)

Gabapentin:
Use: neruropathic pain
Mech: binds to subunit of voltage gater Ca channel

Pregabalin: Same as gabapentin (but higher affinity)

                               Gabaergic Drugs
Phenobarbital:
Use: tonic clonic
Mech: opens cl- channel to inactivate entire cell

                                 Na/Ca/Gaba
Topiramate:
Use: partial seizures
Mech: GABA, blocks AMPA, blocks NA channels

Felbamate:
Use: tonic clonic, partical seizures
Mech: NMDA receptor
                                Psycosis
(Parkinson)Da release from s. nigra (D2 receptor caudate) = inhibits
movement

(psycosis) Da = frontal cortex neurotransmitter
-motor side effects due to D2 antagonists

                           Typical Antipsycotics
Thioridazine
- High sedative / High anticholenergic = low motor side effects
- D2 antagonist

Haloperidol
- D2 selective antagonist
- low sedative/ low anticholenergic = High motor side effects

                          Atypical Antipsycotics
Risperidone
- “Atipical”
- strong 5HT2 antagonist, strong d2
- less side effects than typicals

Clozapine
- “Atipical”
- Strong 5HT2 antagonist, weak d2
- Motor side effects
* Agranulocytosis

Olanzapine
- “Atipical”
- strong 5HT2 (serotonin) antagonist, weak D2
-No motor side effects\
- used instead of clozapine (No agranulocytosis)

Aripiprazole
- “Atipical”
- New antipsychotic
- D2 Agonist (lowers nigra dopamine release),
  D2 Antagonist (post synaptic straital)
- No Motor side effects
                             Parkinsons
-(Parkinson)Da release from s. nigra (D2 receptor (caudade)=inhibit motion
suppression -= movement
-Ach + glutamate(caudate)= activate movement suppression= no movement
                          DA replacement Drugs
L dopa + carbidopa (sinemet)
- Dopamine substitute (kinda)
- side effects: orthostatic hypotension, dyskinesia

Entacapone
- blocks l-dopa metabolize in blood
- extend life of (sinemet)

                             Anticholenergics
Benzatropine
- enhance motion
-Early PD
- low TI
* side effect = SLUD
                               DA Agonists
Bromocriptine
- D2 receptor agonist, early and late PD
- side effect = fibrosis, hallucinations

                               Misc Drugs
Amantadine
-new antiviral
-enhances DA release(s. nigra), block glutamate and ACH in
caudate)

Selegiline
- inhibits DA metabolism (stays in brain longer)
- side effect = reacts w/ SSRI‟s and tricyclics
-mild effects and expensive

Apomorphine
-rescues “frozen” person
-powerful d1/d2 agonist

Benzos
- reduce tremors
                         Autonomic Drugs
                           Muscarinic Agonists
- parasympathetic (AHC release)
- cause vasodilation via NO receptors
-side effects; DUMBBLES

Pilocarpine: used to stimulate salivary flow for patients w/xerostomia
Cevimeline: used to stimulate salivary flow for patients w/xerostomia
Bethanechol:

                      Indirectly acting cholinomimetics
- inhibitors of anticholinesterases (cause build-up of ACH)
- affects PNS, SNS, skeletal muscle
- reverse neuromuscular junction blockers

Donepezil: Alzheimer‟s treatment
Neostigmine: myasthenia gravis treatment (no brain entry)
Physostigmine: uncharged at in body (can get into brain
- treatment of atropine poison ( ACH competes w/atropine for muscarinic
receptor, so, more ACH in terminal means more stimulus)

          Cholinergic Blocking Agents (Muscarinic Antagonists)
- blocks sympathetic postganglionic AHC receptors and sympathetic
muscarinic receptors in sweat glands.
- may cause xerostomia

Atropine/Scopolamime: CNS effects of parkinson‟s disease
Ipatropium/Tiotroipium: COPD patients, decrease secretions
Tolterodine: incontinence
Diphenhydramine: OTC sleep aid, antihistamine, motion sickness treatment

                    Neuromuscular Junction Blockers
- block ACH effect on skeletal muscle
- barroreceptor mediated heart rate changes blocked

Nicotine
Varenicline: smoking cessation (partial nicotine agonist=can act as
antagonist)
- side effects= nausea, vomiting
Mecamylamine: blocks ganglionic transmission (smoking cessation)
- orthostatic hypotension, xerostomia
                      Sympathomimetic Agents
Epinephrine: A1, A2, B1, B2
Norepinephrine: A1, A2, B1
Isoproterenol: B1, B2
Dopamine: D1, D2 (A1, B1 in high doses)

Agents acting directly on adrenergic receptors

Phenylephrine: A1 agonist
- Vasoconstriction, pupil dialation
- used in local anesthetics (vasoconstrictor) *safer for cardiac patients
- metabolized by MAO (don‟t use w/patients taking MAO inhibitors)

Levonordephrine (Clonidine and alphaphamethyl norepinephrine): A2
agonist
- acts on CNS vasomotor center (decrease sympathetic output)
- hypotension, sedation, Vasoconstriction (peripheral blood vessles)

Dobutamine: B1 agonist
- stimulate cardiac tissue (increase heart rate

Albuterol: B2 agonist
- relaxation of vascular, bronchiole, uterine smooth muscle
- acute asthma treatment

Salmetrol: B2 agonist
- chronic asthma treatment (slow acting and long-term)

Dopamine: Multi receptor agonist
- increase cardiac output (B1 activity)
- increase kidney arteriole vasodilation

Indirectly acting agents:

Amphetamine and Tyramine
- act via NE realease (can get into CNS, unlike injected NE)
                                Sympatholytics
- occupy receptor, but lack efficacy (don‟t elicit response)

Alpha Adrenoceptor Antagonists

Prazosin + Tamsulosin
-block effects of endogenous NE and EPI
-decrease vascular resistance (easier for heart)
- increase urinary outflow
- block A1 vasoconstrictors (levonordefrin)
*Orthostatic hypotension

Beta Adenoceptor Antagonists
- reduce cardiac output
- may result in bronchiole constriction (aggravate asthma)

Propranodol: non-selective beta receptor blockers
Metoprolol: selective B1 blocker
Carvedilol: A1 and Beta receptors

Agents acting sympathetic nerve endings
- can be sympatholytics or sympathomimetics

Guanadrel/Bretylium/Reserpine: inhibit nerve action potential, inhibits
storage of NE in vesicles (sympatholytic)
- general loss of SNS
* Orthostatic hypotension

Cocaine: blocks reuptake of NE (sympathomimetic)

MOA inhibitors: decrease NE biosynthesis, decreased SNS function
* orthostatic hypotension
- Don‟t take w/tyramine (= sudden release of NE = Very high BP)
                          Antidepressants
- receptor desensitization takes several weeks (body rebounds to decrease
receptor #)

Clomipramine: Tricyclic, Unipolar depression, OC disorder
-NE reuptake inhibitor/desensitize receptor
- side effects: orthostatic hypotension, SLUD, dry mouth
* interacts w/sedatives

Phenelzine: MAO inhibitor, Unipolar depression
-blocks breakdown NE, 5HT, DA/desensitize receptors
- side effects: convulsions if OD
* Don‟t take w/tyramine foods, antihistamine, decongestant = hypertension
crisis

Sertraline SSRI, Unipolar depression
- selective serotonin (5HT) reuptake inhibitor/desensitize receptors
- side effects: safe anti depressant (can‟t really OD)

Venlafaxine: SNRI, Unipolar depression (take 2-3x daily)
- serotonin/NE, desensitize receptors
- side effects: hypertension (mild)

Buproprion: Atipical, unipolar depression and psychomotor
retardation/nicotine addiction
- Dopamine/Seratonin reuptake inhibitor/desensitize receptor
- side effects: nervousness/insomnia, don‟t react well with other sedatives

Lithium: Bipolar depression/Mania
-modifies NE and 5HT transmission
-side effects: muscle fatigue, ataxia
* NSAIDs reduce renal excretion of Li (toxic)
                       Anxiolytic-Sedatives

- most act on GABA receptor    the brains main inhibitor (cl- channel)

                               Benzodiazapine
- Dose dependent CNS depressants
- Anxiety drug of choice
- safe alone but lethal w/booze
- long acting = hangover (metabolites can be active and longer lasting than
original drug)
- short action = rebound

Oral Benzo‟s
Triazolam: short term pre-surgical sedatio
- oral benzo (short term 2-hrs)
- rebound anxiety
Alprazolam: anxiety/insomnia
- medium lasting oral benzo ( 6-20 hrs )
Diazapam: anxiety and Insomnia
- Oral benzo (long lasting 14-90 hrs)
- no cardiac or respitory depression
- side effects: dependence with long term use


Midazolam: preanesthetic sedation (dentistry)
- short acting/water soluble IV benzo (GABA receptor agonist)
-no major respitory/cardiac depression
-rebound anxiety/insomnia when drug wears off

Flumazenil: Benzo reverser (brings patient out of Benzo sedation)
- GABA receptor antagonist
                                    Barbituates
Thiopental: short-term surgical anesthesia
- ultra short acting barbiturate (lipid soluble = enters brain fast then enters fat
stores)
- major respitory and cardiac depression in OD, hangover intoxification
(leach from fat stores)

Secobarbital: short-term insomnia
- intermediate acting oral barbiturate (GABA agonist)
- side effects: diminishing TI over time (tolerance to ED, not LD), hangover
effect, physical withdrawal and dependence from long-term use

Phenobarbital: Epileptic seizures w/o tolerance
- long acting oral barbiturate (GABA receptor agonist)
- slowly metabolized by liver = long lasting
- side effects: major respitory and cardiac depression in OD
                                Other” Sedative
Diphenhydramine/Hydroxyzine: Insomnia, runny nose
- anticholinergic action
- no side effects

Meprobamate: Anxiety/Insomnia
- Barbituate-like action, but can‟t produce surgical anesthesia
- “50‟s women sedatives (Stepford Wives)
- side effects: Low TI

Chloral Hydrate: Liquid sedative (mild anesthetic)
- rapid onset, short duration
- side effects: Low TI
* used for child dental appts

Nitrous Oxide: Anesthesia
- no cardiac or respitory suppression

Melatonin: Insomnia, Jet lag
- mild hypnotic, changes circadian rhythm
                          Non Sedating Anxiolytic
Buspirone: anxiolytic effect only (no sedation), takes several weeks to work
- 5HT agonist (reduces transmission)
- no major effects

Zolpidem: Z Drug. Insomia only
- act on GABA receptor (like benzos)
- side effects: mild psych dependence
* Do not take z-drugs w/ Benzos = bad mix

				
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