Pharm Winter FInal Flashcards
Polyene macrolides
Amphotericin B
Nystatin
Liposomal membrane
Amphotericin B
Amphotericin B mechanism
Binds to sterols in fungal cell membrane
Must give parenterally
Amphotericin B
Causes nephrotoxicity and anemia from decreased erythropoietin release
Amphotericin B
Treats leishmaniasis, amebic meningoencephalitis and other protozoal infxns
Amphotericin B
Imidazoles
Miconazole
Ketoconazole
Triazoles
Itraconazole
Fluconazole
Azole mechanism of action
Inhibit sterol 14 alpha demethylase (a cytochrome p450 enzyme) in ergosterol synthesis causing buildup of lanosterol
Side effect from inhibiting steroid biosynthesis resulting in gynecomastia
Ketoconazole
Drug interactions by inhibiting P450 3A4 enzyme
Ketoconazole
Inhibits Cyt P450 thus affeting metabolism of cyclosporine, rifampin, and warfarin
Fluconazole and Itraconazole
Treats cryptococcal meningitis and oropharyngeal and vaginal candidiasis
Fluconazole
No parenteral formulation available
Itraconazole
Griseofulvin
Griseofulvin MOA
Disrupts mitotic spindle structure arresting metaphase of cell division
Deposited in keratin precursor cells
Griseofulvin
Ultramicrosize absorbed better
Griseofulvin
Only used for dermatophytoses (tineas) except tinea versicolor
Griseofulvin
Nystatin MOA
Binds to sterols in the fungal cell membrane
Too toxic for parenteral use
Nystatin
Nystatin is used for what
Candidal infxns
Tolnaftate MOA
Inhibits squalene monooxygenase leading to squalene accumulation
Mainly used against dermatophytoses (doesn’t say onnly for this though…)
Tolnaftate
Terbinafine
Terbinafine MOA
Inhibits squalene monooxygenase leading to squalene accumulation
Echinocandin
Caspofungin
Caspofungin MOA
Inhibits synthesis of Beta 1,3 D glucan into polysaccharite cell wall
Use of casponfungin
Aspergilloma and Esophageal Candidiasis
If given with cyclosporine, increased plasma levels
If given withinducers of drug clearance, decreased plasma levels
Caspofungin
Alternative to Ketoconazole since less toxic
Fluconazole
Alkylating agents
Mechlorethamine
Cyclophosphamide
Carmustine
Cisplatin
Antimetabolites
Methotrexate
Mercaptopurine
Fluorouracil
Cytarabine
Natural products
Daunorubicin Doxorubicin Vinblastine Vincristine Etoposide Paclitaxel
Hormonal agents
Prednisone
Dexamethasone
Tamoxifen
Kinase inhibitors
Imatinib
Monoclonal antibodies
Trastuzumab
Developed from mustard gas
Mechlorethamine
Cyclophosphamide
Nitrosureas
Carmustine
Platinum complexes
Cisplatin
Alkylating agents MOA
Damage DNA by transfering reactive alkyl groups to N7 guanine position
Causes DNA breaks and crosslinking of DNA
Requires metabolic activation by Cyt P450
Cyclophosphamide
Used for brain tumors
Carmustine
Nephro and Ototoxic
Cisplatin
Folic acid analog
Methotrexate
Methotrexate MOA
Inhibits dihydrofolate reductase
Cell cycle specific agents
Antimetabolites
What phase does Methotrexate effect
S phase
Used for psoriasis and RA
Methotrexate
Purine analogs
Mercaptopurine
Inhibits a number of enzymes of purine interconversion
Mercaptopurine
Converted to nucleotide form by HGPRT
Mercaptopurine
Metabolized by xanthine oxidase
Mercaptopurine
Inhibits xanthine oxidase
Allopurinol
Pyrimidine analogs
Fluorouracil
Cytarabine
Fluorouracil MOA
Inhibits Thimidylate synthetase in DNA synthesis
Cytarabine MOA
Inhibits DNA polymerase
Cancer antibiotic drugs/Anthracyclines
Daunorubicin
Doxorubicin
Daunorubicin and Doxorubicin MOA
ind to DNA between adjacent strands uncoiling DNA helix
Tetracycline ring gives antitumor activity
Daunorubicin
Doxorubicin
Dilated cardiomyopathy side effect
Daunorubicin
Doxorubicin
Used for acute non lymphocytic leukemia
Daunorubicin
How does vinblastine differ from vincristine
Vinblastine has methyl group
Vincristine has formyl group
What cell cycle stage is targeted by vinblastine and vincristine
Mitosis
Vinblastine/Vincristine MOA
Bind to tubulin of Microtubules leading to metaphase arrest
Etoposide MOA
Complexes with Topoisomerase 2 resulting in DNA breaks
Etoposide targets what phase of cell cycle
G2
Alopecia side effect
Etoposide
Paclitaxel
Paclitaxel MOA
Promotes microtubule assembly (Antimicrotubule)
What phase does paclitaxel target
G2 and M
Adrenocorticosteroids
Prednisone
Dexamethasone
Cushing Syndrome side effect
Prednisone
Dexamethasone
Antiestrogen
Tamoxifen
Tamoxifen MOA
Inhibits estrogen binding to estrogen receptors
Side effects are menopausal symptoms of hot flashes
Tamoxifen
Most frequently used hormonal therapy for men with breast cancer
Tamoxifen
Imatinib MOA
Inhibits Bcr Abl Tyrosine Kinase formed from Philadelphia chromosomal translocation in CML
Humanized IgG1 monoclonal natibody
Trastuzumab
Trastuzumab MOA
Binds Human epidermal growth factor receptor down regulating the receptors tyrosine kinase signaling
Trastuzumab effects what stage of cell cycle
G1
First line treatment of HER2 breast cancer
Paclitaxel
Trastuzumab
Which alkylating agent is lipid soluble
Carmustine
Pancytopenia side effect
Cytarabine
Increases risk of endometrial cancer
Tamoxifen
ADHD
Lesdexamfetamine
Methylphenidate
Resistant to metabolism by MAO
Methamphetamine
Marketed as bath salts from mostly East Africa and Arabic countries
Cathinone
Ephedrine main use
Sympathomimetic agent
Traeats narcolepsy and shift work disorder
Modafanil/Armodafanil
Amphetamine functions
Stimulates reticular activating system promoting arousal and wakefulness. Suppresses appetite
Sympathomimetic in periphery
Amphetamine toxicities
Cardiac from sympathomimetic effx
CNS effx include hostility, aggression, psychosis, and tactile hallucinations
Amphetamine MOA
enhances release and inhibits uptake of NE and DA
Chronicaly use causes reduced dopamine in cleft
Amphetamines and Cocaine
What has paradoxical effects in the brain to stimulate catecholamine release thus treating ADHD
Amphetamines
Can be used as a local anesthetic with vasoconstriction
Cocaine
Increases confidence and reinforcement
Cocaine
Withdrawal results in lethargy, fatigue, and depression
Cocaine
Teratogenic effects
Cocaine, THC
Cocaine MOA
Inhibits DA reuptake
Methylxanthines
Caffeine, theophylline, aminophylline
Amphetamine drugs
Amphetamine Lisdexamfetamine Methamphetamine Methylphenidate Cathinone Ephedrine Modafenil
Treats asthma
Theophylline and Aminophylline
Respiratory stimulant in preterm infants
Methylxanthines
Stimulates gastric secretion so gotta becareful using in peptic ulcer dz patients
Methylxanthines
Diuretic effect
Methylxanthines
Dilation of vascular beds
Methylxanthines
Methylxanthine overdose pt will present like what
seizures
What is the MOA of methylxanthines
Inhibits phosphodiesterase
Blocks adenosine receptors
Release of Ca
Spinal cord stimulatns
Strychnine
Tetanus toxin
Strychnine MOA
Antagonist at glycine receptors
Use results in seizures
Strychnine
Tetanus toxin
Tetanus MOA
Inhibits release of glycine from renshaw cells
Treats apnea in preterm infants
Caffeine
Theophylline
What is the active ingredient in marijuana
Tetra hydrocanacinol (THC)
What is very lipid soluble and thus easily gets to the brain
Tetra hydrocanacinol
Reddening of the conjunctiva is suggestive of what
THC
Treats glaucoma
THC
Inhibits vomitingg reflex
THC
What are the side effx of cannabinoids
Suppresses immune fxn Lowers testosterone Teratogenic Amotivational syndrome Lung damage
Which has tolerance and sensitized feelings with chronic use
Marijuana
Prevents wasting in AIDS patients
Cannabinoids
MOA of Salvia
Agonist at kappa opioid and D2 dompamine receptors
What is abused for its hallucinogenic effx
Salvia
What serves as a stimulant and pain reliever
Kratom
Kratom MOA
Agonist at mu opioid receptors
Controls opioid withdrawal symptoms
Kratom
Treats Alzheimers
Rivastigmine Donepezil Memantine Vitamin E Selegeline/Deprenyl
Treats ALS
Riluzole
Treats ADHD
Methylphenidate
D amphetamine
Adderall
Atomoxatine
Acetylcholinesterase inhibitors
Rivastigmine
Donepezil
What is the problem in Alzheimers
Loss of Ach producing neurons in the frontal cortex and nucleus basalis of Meynert
What is the problem with the acetylcholinesterase inhibitors
Cholinergic side effx
Memantine MOA
Blocks excitatory actions of glutamate at NMDA receptors in the hippocampus and frontal cortex
Antioxidants
Vitamin E
Selegiline/Deprenyl
Orphan drug
Riluzole
Riluzole MOA
Inhibits the release of glutamate from nerve endings
Mild stimulant
Methamphetamine
Powerful stimulant
Amphetamine
Mixture of amphetamine salts
Adderall
Atomoxatine MOA
Inhibits synaptic reuptake of NE
Non stimulating ADHD drug
Atomoxatine
Side effx of Atomoxatine
Hepatotoxicity
Indoles
Lysergic and diethyamide
Psilocybin and Psilocin
Bufotenin
Ibogaine
Phenylethamines
Mescaline
Methylenedioxymethamphetamine
Hallucinogens
Lysergic and diethyamide Psilocybin and Psilocin Bufotenin Ibogaine Mescaline Methylenedioxymethamphetamine
What are the initial signs of LSD use
Sympathomimetic stuff
What are the more slowly developing signs of LSD
Hallucinogenic effects
What is the side effect of LSD
Bad trip (panic reactions)
Found in mushrooms
Psilocin and Psilocybin
Bufotenin
Toad licking
Bufotenin
Autonomic changes are more pronounced than LSD
Mescaline
Halucinogenic and stimulant
MDMA
Powerful hallucinogen
Ibogaine
Suppresses craving for heroin, cocaine, and other drugs
Ibogaine
Displays cross tolerance
Hallucinogens
No physical withdrawal syndrome
Hallucinogens aside from MDMA
Flashback side effects
Hallucinogens
Long term difficulty with processing visual information
Hallucinogen Persisting Perceptiong Disorder (HPPD)
Anesthetics
Phencyclidine
ketamine
Makes you feel no pain
PCP/Ketamine
Rage reactions
PCP/Ketamine
Signs of acute PCP/Ketamine poisoing
Hyperreflexia Increased muscle tone Hypertension Vertical nystagmus Convulsions
PCP/Ketaine MOA
Blocks NMDA receptors