Spring 2013 Pharm review for Reddy Flashcards
Name the Excitatory NT in the CNS
Glutamate, Substance P
- dopamine, serotonin, NE, Ach depending on the receptor involved
Name the Inhibitory NT in the CNS
GABA, Enkephalins, Glycine (SC)
- dopamine, serotonin, NE, Ach depending on the receptor involved
What are the four dopaminergic pathways in the brain
- Nigrostriatal System
- Mesolimbic System
- Mesocortical System
- Tuberinfidibulum System
The Nigrostriatal system regulates
movement
The Mesolimbic system regulates
emotion, love
The Mesocortical system regulates
cognition, motivation
The Tuberinfindibulum system regulates
pituitary
Dopamine, NE are both released at nerve terminals, How is the action of these NT terminated
- Reuptake (about 90%)
- MAO-metabolism
- COMT-metabolism
Name three drug strategies to increase the amount of NT
- Inhibit reuptake
- Inhibit MAO
- Inhibit COMT
Name two examples of drugs used to inhibit NT reuptake
cocaine
TCA- Imipramine
Name a drug used to inhibit MAO
Selegiline
*used in alzheimer’s dx to inhibit MAO B
Alzheimer’s is characterized by loss of many neurons, especially
cholinergic
*Too little Ach
Alzheimer’s results in impairment of
memory and cognitive functions
Name a drug used to increase AcH in the brain
Donepezil
What NT is implicated in destruction of cholinergic nerve death
Glutamate
What drug is used to address glutamates effect on patient’s with alzheimers
Memantine
Attention-deficit/Hyperactivity disorder is characterized by
Persistent pattern of frequent, severe inattention and/or hyperactivity
What drugs are most frequently used to tx ADHD
stimulants
What secondary drug is used to tx ADHD
nonstimulant
- Atomoxetine- given to patient’s refractory to stimulant therapy
Atomoxetine is a
selective NE reuptake inhibitor
Name two stimulants used to tx ADHD
methylphenidate (ritalin)
amphetamine (adderrall)
- both work in RAS
methylphenidate’s MOA includes
blocking reuptake of dopamine in CNS
amphetamine’s MOA includes
increases release of dopamine & NE
Name the three main drug categories used to tx anxiety
- Benzodiazepine
- Non-Benzo Benzos
- Buspirone
Benzos agonize what receptor
GABA
- opens chloride channels
Non-Benzo benzos agonize what receptor
GABA
Name some benzos
“zepam” or “zolam”
Diazepam, Lorazepam, Midazolam
Buspirone partially agonizes what serotonin subtype
5-HT 1A
What is the difference b/t Buspirone and Benzos
Benzos onset immediate
Buspirone onset takes weeks
Buspirone increases risk for seizures, increased HR (stimulant)
Non-Benzo benzo’s major difference from Benzos is that
it is less addictive
Name three major non-benzo benzos
Zolpidem
Zaleplon
Eszopiclone
What is the GABA antagonist used to treat overdose of benzos and non-benzo benzos
Flumazemil
Name a drug used to inhibit COMT
**capone
What two drugs help with insomnia
Melatonin (released by pineal gland)
RaMELTeon
Parkinson’s is characterized by
too little dopamine in the nigrostriatial pathway
What 1st line drug combination is used to tx parkinsons
levadopa and carbidopa
Why is carbidopa added to L-dopa therapy
to inhibit L-aa carboxylase from converting L-dopa to Dopamine in the periphery
What is the on-off phenomenon seen with parkinson treatment with L-dopa/carbidopa
normal movement followed by resting tremors, rigidity, bradykinesia, etc
- caused by continued loss of dopamine neurons
Name three other strategies besides replacing dopamine used to tx parkinsons
block metabolism of dopamine
dopamine agonism
anti-Ach drugs
name two drugs used to block dopamine metabolism via inhibition of COMT
talCAPONE
entaCAPONE
name a drug used to block dopamine metabolism via inhibition of MAO
selegiline (MAO B)
Name a dopamine agonist used to tx parkinsons
Bromocriptine
Name an anti-cholinergic drug used to tx parkinsons
benztropine
Huntington’s disease is characterized by loss of
GABA neurons- loss of inhibition
*Too much movement (chorea)
What is the tx strategy for Huntington’s disease
control symptoms, support therapy
List the four primary drugs used to tx epilepsy
Valproic acid
Ethosuximide
Phenytoin
Carbamazepine
Name the generalized seizures
Generalized tonic-clonic (grandMal)
Absence (PetitMal)-originating in occipital area
Myoclonic (muscle involvement)
Name two drugs used to treat generalized tonic-clonic seizures
carbamazepine
valproic acid
Name two drugs used to tx absence seizures
Ethosuximide-blocks ca2+ current in thalmus
valproic acid
Name the three partial seizures
simple partial - No LOC
complex partial - LOC
partial seizures with secondary generalization
Name a drug used to tx all three partial seizures
carbamazepine
What is the MOA of most antiepileptic drugs
blocking or hyperpolarizing ion channels
What two antiepileptics work by blocking sodium channels
Carbamazepine
Phenytoin
What two antiepileptics work by blocking calcium channels
Ethosuximide
Valproic acid
What four antiepileptics work by hyperpolorizing neurons
Carbamazepine
Benozs
Phenobarbital
Valproic Acid
Name two other strategies used to tx epilepsy
enhancement of GABA
reduction of excitatory NT
Name four SSRI used to tx depression
Fluoxetine
Sertaline
Citalopram
Escitalopram
Name four TCAs used to tx depression
Amytryptiline, Nortryptiline
Imipramine, Clomipramine
TCAs MOA is
nonspecific blockers of serotonin and NE
Why is SNRI considered better than TCAs even though they both target the same transporters
SNRIs have no SE common to TCAs
What are the SE of TCA administration
Anticholinergic- urinary retention, dry eyes, constipation, dry mouth
Antihistamine- sedation
alpha 1 blockade-dizziness, orthostatic hypotension
What are cholinergic AE
DUMB BELSS
D-Diarrhea U-Urination M-Miosis B-Bradycardia E-Excitation (CNS & Skeletal muscles) L-Lacrimation S-Salivation S-Sweating
Schizophrenia is characterized by
too much dopamine in the mesolimbic system
List the Positive symptoms of schizophrenia
Hallucination
Delusions
Bizzare behavior
List the Negative symptoms of schizophrenia
Affective flattening - dec. in emotional expression
Alogia- decr. in fluency in speech
Avolition- decr. in goal-oriented behavior
What are the strategies used to tx schizophrenia
Block dopamine receptors
Block Acetylcholine receptors
Block alpha receptors
Block Histamine receptors
What are the AE associatesd with tx of schizophrenia
face/neck muscle spasms (tx with antichol)»Akathisia (motor restlessness)»>parkinsonism»»tardive dyskinesia
Name two “typical” antipsychotics
Chlorpromazine
Haloperidol
- Possess more extrapyramidal SE than atypical
- Strictly blocks D2 receptors
Name two “atypical” antipsychotics
Clozapine
Risperidone
What is the advantange of using atypical antipsychotics
D2 and 5 HT blockers
Atypicals block the inhibitory 5-HT 2A (presynaptically) in the nigrostriatal pathway and mesocortical pathways yielding less extrapyramidal SE and improvement of negative symptoms
How does adding 5-HT antagonism improve the antipsychotics
By reducing the SE- mostly motor and endocrine
What is Neuroleptic Malignant Syndrome
is a life-threatening neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs
- dopaminergic system in hypothalamus is disturbed. Loss of ability to control temperature
What are symptoms associated with NMS
F – Fever A – Autonomic instability L – Leukocytosis T – Tremor E – Elevated enzymes (elevated CPK) R – Rigidity of muscles
How is NMS treated
Supportive care
Dantrolene- Skeletal muscle relaxant
Bromocriptine-DA receptor agonist
What is Atomoxetine
Non-stimulant drug used to tx ADHD that blocks NE reuptake and is given to patients who cannot tolerate stimulants
What is Benztropine
Benzatropine is a centrally acting anticholinergic/antihistamine agent used in the tx of Parkinsons
What is Entacapone
COMT inhibitor used sometimes in patient’s tx for Parkinsons to prevent degradation of L-Dopa or Dopamine
What is Eszopicclone
Eszopiclone is a short acting nonbenzodiazepine sedative hypnotic used to tx anxiety or insomnia
What is Duloxetine
SNRI used to tx depression
What is Enfuviritide
HIV fusion inhibitor
What is Fluoxetine
SSRI used to tx depression
What is Flumazenil
Benzodiazepine antagonist used to reverse overdose of benzos/nonbenzos.
What is Lamotrigine
Antiepileptic
What is Memantine
used in the tx of Alzheimers to act on the glutamatergic system by blocking NMDA-type glutamate receptors.
*Glutamate neurons thought to play a role in cholinergic neuron destruction
What is Oseltamivir
is an antiviral drug, which may slow the spread of influenza (flu) virus
What is Ramelteon
Drug used to tx insomnia (Melatonin-like)
What is Rifampin
A bacteriocidal drug that inhibits bacterial DNA-dependent RNA synthesis by inhibiting bacterial DNA-dependent RNA polymerase
What is Amphoteracin B
A polyene macrolide antifungal drug that binds with ergosterol, a component of fungal cell membranes, forming a transmembrane channel that leads to monovalent ion (K+, Na+, H+ and Cl−) leakage, which is the primary effect leading to fungal cell death
*Broadest antifungal spectrum so often used as first choice for mycotic infections
What is Metronidazole
Mixed amebicide (luminal and systemic tx) for treating protozoal or bacterial infections
- Prodrug that must be acitvated once inside pathogen cells
- Activating enzyme= Nitroreductase found ONLY in anaerobic organisms
- Once induced, it inhibits DNA replicaton and kill cells
*Tx: Trichomoniasis, Ambiasis Giardiasis M-(TAG)
What is Mebendazole
Used to treat Nematodes (round, whip, pin,hook, ascaris worms) found in GI tract by interfering with microtubules and blocking glucose uptake- Worm can’t move and has no energy»>defecated out in feces
What is Terbinafine
Antifungal drug used to tx dermatophytes by inhbiting squalene epoxidase and decreasing ergosterol syntheis
What is Donepezil
a centrally acting acetylcholinesterase inhibitor. Its main therapeutic use is in the palliative treatment of Alzheimer’s disease
What is Echothiophate
Irreversibly binds to plasma cholinesterase. Once bound, the enzyme is permanently inactive and the cell has to make new enzymes
What is Artimisinin
Antiprotozoa drug used to tx the most severe and resistant form of malaria caused by Plasmodium Falciparum
*Targets Blood schizonides
What is Chloroquine
Drug of choice for prophylaxis and tx of uncomplicated attacks of malaria. It binds to heme, preventing its growth in RBC resulting in membrane damage and cell lysis
What is Pyrimethamine
Antiprotozoa drug used to tx malaria by inhibiting folate needed for DNA/RNA synthesis
What is Quinine
Antiprotozoal drug used to tx malaria by interfering with polymerization (growth) within heme
What is Sulfadoxine
is an ultra-long-lasting sulfonamide often used in combination with pyrimethamine to treat or prevent malaria by interfering with folate synthesis
What class is Azithromycin
protein synthesis inhibitor
What class is Cefuroxime
second generation cephalosporin
What class is Ciprofloxacin
Inhibits bacterial DNA synthesis
What class is Sulfamethoxazole
inhibits folate synthesis
What class is Tobramycin
Aminoglycoside that inhibits protein synthesis
What class is Vancomycin
Glycopeptide that inhibits cell wall synthesis
What class is Linezolid
Protein synthesis inhibitor
What class is Rifampin
RNA syntheis inhibitor
What is the function of adding Clavulonic acid to amoxicillin (Augmentin)
Clauvulonic acid B-lactamase while amoxicillin (PCN) inhibit cell wall biosynthesis
T/F- Most first generation cephalosporins begin with “ceph”
True
What is post-antibiotic effect
Long after antibiotic is administered, effects linger
Name a drug or class that exhibits post-antibiotic effects
Aminoglycosides
*Oto, nephro, neuro toxic
Name the four mechanism of drug resistance
- Alter their metabolic pathway
- Alter target protein (enzyme)
- Alter target site
- Decreased membrane permeability
Drugs used to tx herpes infections are classifed as
Nuceloside analogs VS. Non-nucleoside analogs
What drug class is most effective for tx herpes
Nucleoside analogs
Name two nucleoside analogs
Acyclovir
Ganciclovir
Name a non nucleoside analog
Foscarnet
What anti-viral is most effective at treating respiratory infections
Ribivarin
*PalvizuMAB: monoclonal antibiody used tx
What is the reason for combination tx for HIV
Therapy with RT inhibitors and Protease inhibitors can reduce the emergence of resistance and produce additive effects
What are the classes of drugs used to tx HIV
Reverse Transcritase inhibitors
Protease Inhibitors
Fusion Inhibitors
Integrase Inhibitors
Reverse Transcriptase Inhibitors are further classified as
Nucleoside inhibitors
Nonnucleoside inhibitors
Name three nucleoside RT inhibitors
Didanosine
Abacavir
Zidovudine
Name one nonnucleoside RT inhibitor
Efavirenz
Name two protease inhibitors used to tx HIV
Indinavir
Ritonavir
“NAVIR”
Name two fusion inhibitor used to tx HIV
Maraviroc
EnFuviritde
Name one integrase inhibitor used to tx HIV
RalTEGravir
What is the drug of choice to tx Giardia (common cause of diarrhea)
Metronidazole
What is the drug of choice to tx big round worms found in stool
Mebendazole
Albendazole
Name two drugs used to tx Influenza A
Amantadine
Rimantidine
*must be started within 48 hours to be effective
Name two drugs used to tx Influenza A & B
Zanamivir
Oseltamivir (Tamiflu)
- If given within 30 hours of onset of flu, both drugs can shorten the duration of illness
- Neuramindase inhibitors that are prophylactic for flu
Zanamivir is given via what route
Inhalation ONLY
Oseltamivir is given via what route
Orally
What drug is used to treat Parkinsons as well as Influenza
Amantadine
- blocks NMDA receptor>Incr. glutamate
- Txs Influenza A
What Cancer drug is unique for targeting cancer-specific tyrosine kinase
Imatinib (Gleevec)
How does Imatinib work
works by preventing a central tyrosine kinase enzyme, in this case BCR-Abl, from phosphorylating subsequent proteins and initiating the signaling cascade necessary for cancer development, thus preventing the growth of cancer cells and leading to their death by apoptosis
What is the major AE of Cyclophosphamide
Myelosuppression-rate limiting
*alkylating agent (N. Mustard)
What is the major AE for Methotrexate
Myelosuppression-rate limiting
- Antimetabolite-Inhibits folate
What is the major AE for Taxol
Myelosuppression-rate limiting
*binds to tubulin PREVENTING microtubule disassembly
What is the major AE for Doxorubicin/Daunorubicin
Cardiotoxicity
*Anthracycline: intercalating agent that inserts b/t DNA base pairs
What is the major AE for Cisplatin
Renal toxicity
*Platinum Coordination Complexes with DNA (guanine)
What is the major AE of Vincristine
neurotoxicity
- binds to microtubule and blocks assembly
Give an example of combination chemotherapy
CHOP
C-cyclophoshamide (crosslinks DNA)
H-Hydroxydaunorubicin (Intercalates with DNA)
O-Oncovin(Vincristine)(mitotic spindle poison)
P-Prednisone (anti-inflammatory steroid, binds tubulin)
Name receptors involved in N/V with anti-cancer drugs and the drugs used to antagonize them
5 HT 3 (ondansetron) D 2 (Promethazine) & Phenothiazine
*Phenothiazine should be avoided in patient’s with Parkinson’s disease