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349 Cards in this Set

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Vincristine
Vinca alkaloid natural product against cancer. Terminates mitotic spindle assembly by binding to tubulin.

Toxicity: constipation, orthostatic hypertension, urinary retention, CNS problems.

Resistance: alteration in tubulin bind, upregulation of P-glycoprotein which sends drug out of cell.

Pneumonics: C-CNS
Vinblastine
Vinca alkaloid natural product against cancer. Terminates mitotic spindle assembly by binding to tubulin.

Toxicity: constipation, orthostatic hypertension, urinary retention, Bone Marror problems.

Resistance: alteration in tubulin bind, upregulation of P-glycoprotein which sends drug out of cell.

Pneumonics: B-Bone Marrow
Paclitaxel
bind to tubulin and promote ASSEMBLY to mititoc spindle. (Beta Site) (AGAINST CANCER)

Toxicity: neuronal and Bone Marrow

Resistance: alteration in tubulin bind, upregulation of P-glycoprotein which sends drug out of cell.
Which Vince Alkaloids (1)Inhibit mitotic spindle and Which ones (2) Promote mitotic spindle?
1) Vincristine/Vinblastine
2) Paclitaxel
Epipodophylotoxins
Block stage G2 for Cancer (Plant Alkaloid) and Inibit TOPOISOMERAS 2

Resistance: P-glycoprotein
Commonalities of antibiotics used for cancer
all products of streptomyces

Mechanisms: 1) large molecules which intercalate in DNA and bind to GUANINE
2) Block RNA Polymerase
3) decrease topoisomerase activity
4) increase Free Radical Production
Major Base that the Antibiotics for cancer bind to
Guanine
Only Antibiotic to be cell-cycle specific and block phase G2
Bleomycins
Patient has a skin or lung cancer (epithelial origin), give them whAT ANTIBIOTIC?
Bleomycins
Bleomycins Specific facts
adverse effect to the lung - pulmonary fibrosis

No overlap of toxicities with other drugs
Used for squamous cell or testicular tumors - Antibiotic
Bleomycins
Anthracyclines
What are they?
Whats their problem
Non-cell cycle specific Cancer Antibiotic

Interact with P450 causing increase in free radicals leading to cardiomyopthy

(Daunorubicin, Doxorubicin, Mitoxantrone)
Mito does not cause free radicals and the adverse effect

They can also cause alopecia
Which anthracyclins does not cause the adverse effect?
Adverse effect = cardiomyopthy

Which one does not? - Mitoxantrone)
Dactinomycin
Antibiotic cancer. used for sarcomas, it is most potent. It is bad with use of radiation
What is the most potent Anti-tumor agent and what is it used for?
Dactinomycin is used for Sarcomas and is?
What is dactinomycin synergistic with?
Radiation
What do u use for advanced testicular tumor?
How does it work?
Plicamycin/Mithramycin (antibiotic cancer)

Impairs clotting factors
antibiotic to reduce calcium secreting tumors
plicamycin
hypoxic tumors you use what?
How does it work?
What are its side effects?
Mitomycin C
it is an alkylating agent
ANEMIA, renal, interstitial pneumonitis
Only active agent n Acute Lymphoblastic Leukemia?

Side effects?
Asparaginase

S.E.: anaphylactic type reactions
A person had a MELANOMA or a HAIRY CELL LEUKEMIA and then on treatment got a FLU, what drug?
Cytokines such as interferons/interleukins augment T-cell cytotoxicity
TX for Non-Hodgkins lymphoma
Rituximab
Rituximab method for killing and adverse effects
binds to CD20 to help with nonhodgkins lymphoma. Can cause hypersensitivity and circulatory problems if used too soon.
Used for Adrenal corticoid tumors
Mitotane
After you have treated with mitotane, what do you give and what type of patient needs it?
Patient with adrenal corticoid tumor...after TX give them replacement hydrocortison because drug can cause side effects of LETHARGY and SKIN ERUPTIONS
Amsacrine
Used for Cancer...Binds to topoisomerase 2 in DNA and can cause cardiac arrest
Adrenocorticosteroids (Prednisone)
For cancer.
1) inhibit Tumor Growth
2) Improve physical health
3) Reduce calcium levels in advanced breast cancer

Cause nausea and vomiting
Aminoglutetimide
1st generation aromatase inhibitor used for breast cancer. it inhibits all adrenal steroidsogenesis, so you need to have a hydrocortisone therapy with it
Anastrozole
3rd gen aromatase inhibitor used for breast cancer. Selectively effects the aromatase enzyme converting androstenedione to estrogen.

Basically it inhibits the prodcution of estrogen in post menauausal women in order to reduce estrogen levels which is proven to prevent breast cancer.
Better breast cancer treatment...Aromatase or a Tamoxifen?
Aromatase like anastrozole is a better initial therapy
Antiestrogen: tamoxifen

Side effects:
binds to estrogen and inhibits transcription

Side effects: increase endometrial cancer, thromboembolic events, hot flashes, nausea
delays onset of osteoperosis
Tamoxifen
Raloxifen
antiestrogen that is safer than tamoxifen
Used in treatment of premenapausal people with high susceptibility to breast cancer
Tamoxifen
treatment of prostate cancer
leuprolide
leuprolide

Side effects:
stimulates release of FSH and LH in pituitary, and initially a flare reaction of increase of testosterone which can be subdued by giving FLUTAMIDE to reduce amount of steroid receptors.

Used for prostate Cancer

SE: gynecomastia, thromboembolism, edema, nausea, vomiting.
Needed to give with leuprolide to reduce initial "Flare up"
Flutamide
mOst Important T-cell growth factor
IL-2
Helper T-cells make these cytokines
IL-4, IL-5, IL-6
Macrophages make these cytokines.

What is 1 of them responsible for?
The first make TNF-a which then makes IL-1 and then IL-6.

TNF-a is responsible for Rheumatoid Arthritis
Cyclosporine
Targets calcineurin in T-cells and does not allow NFAT to go into the nucleus and increase IL-2 transcription.


Needs to be given before the inflammation. Does not cause bone marrow problems

S.E.: liver problems, nephrotoxicity.
FK506
Targets calcineurin in T-cells and does not allow NFAT to go into the nucleus and increase IL-2 transcription. Does not cause bone marrow problems

Needs to be given before the inflammation.
Rapamycin
Targets mTOR (FKBP) and blocks the RESPONSE TO IL-2. Prevents progression from G1 to S. You can give this drug later in the inflammation episode

less nephrotoxicity
Rapamycin combonation
Can take it with Cyclosporin but not with FK506
Azathioprine
anti-metabolite that is a 6-mercaptopurine derivative. Inhibits DNA synthesis on rapidly proliferating cells. needs to be taken with other agents
Corticosteroids in immunotherapy do what 3 things?
1) neutrophillia (increase)/lyphopenia(decrease)/monocytopenia(decrease)
2)functional changes on leukocytes
3)inhibit leukotriens/COX2/IL-1. IL-8, TNF-a
Anti-CD3 Anitbody
used prophylactically to prevent an immune response before organ transplantation
IgG-Anti-Rh(D) (Rhogam)
used for passive immunization and for pregnancy when a child has a different RF factor than the mother
Common feature of NSAIDs
(-) Cox-1 and/or COX-2.
AlL have analgesic, anti-pyretic, anti-inflammatory effects, used to close patent ducturs arteriosus.
Only NSAID not to have an inflammatory effect
Tylenol (Acitomenaphen)
Similar Side effects of NSAIDs (4)
1) GI irratation moreso with COX-1 inhibitors

2) Renal toxicity

3) Sodium and water retention

4) Decreased platlet aggregation with COX-1 inhibition
Aspirin mechanism and Uses
Blocks COX 1 and COX 2 but more selective for COX1 for low doses and equally selective at high doses

IRREVERSIBLE block of COX1 which is needed to convert arachidonic acid intro prostaglandin. So it BLOCKS PLATELET AGGREGATION and reduces COLON CANCER
Aspirin Side Effects
GI tract irritation and ulceration, hemorrhage, and renal toxicity, tinnitus(ringing in ears)
Moderate stage of aspirin overdose
It is an acid so it lowers blood pH which causes a reflex exretion of CO2
Severe Aspirin Overdose
Aspirin is an Acid so pH gets too low and inhibits the respiration center causing metabolic acidoses and low levels of bicarbonate causing HEART FAILUER
Celecoxib

Side Effects
COX-2 inhibitor so they do not affect platelet function. Less GI distress

Increased cardiovascular thrombotic event and renal toxicity
Taken with (this) COX-2 inhibitors to reduce their chances of thrombotic event
COX-2 inhibitor - Celecoxib
Taken with it - Baby aspirin
Acetaminophen location of action
only works in CNS and Spinal Cord and not periphery so do not have gastric problems.
Acitomenaphen side efffect and who should not take them
Liver toxicity
Alcoholics should not take them
What acitomenaphen turns into if it is metabolized by CYP450 instead of glucaronic/sulfuric acid
Benzoquinopomine which can cause cell death
ibuprofen
what is its contraindication?
propionic acid derivative which blocks COX1 and COX2 reversibly and should not be used with people with nasal polyps
Diclofenac
COX-1/COX-2 inhibitor which accumulates in synovial joints

less complaints of GI ulcers
Etodolac
more COX-2 selective and a good painkiller and used after bypass surgery.
Ketoroloac
COX2 inhibitor used for pain killing after surgery especially to reduce use of morphine
Indomethacin
Potent analgesic effect and anti-pyritic effects but used for anti-inflammatory
TX: acute gout and hodgkins fever
What do you use for Hodgkins disease which has a stubborn fever?
Indomethacin
Gout - Cause and Effect
causes arthritis

You get gout usually by excess uric acid which comes from purine degeneration. so Uric Acid builds up and forms crystals in the joints which cause an inflammatory reaction
Tx for gout involves...
1) relieve inflammation (Colchicine)

2)reduce uric acid concentration (Probenecid and NSAIDs)

3)reduce synthesis of uric acid (Allopurinol and Febuxostat)
Colchicine
TX for gout inflammation.

Should be first treatment because it affects polymerization fo microtubules
Reduce Uric Acid absorption in Gout
Probenecid/indomethacin (NSAIDs)
use at high doses because then it blocks reabsorption, but if you use low doses it promotes reabsorption
OAT and URAT
OAT is used for secretion of Uric acid (dnt want to block this in GOUT)

URAT isused for reabsorption of Uric Acid (want to block this in gout)

OAT - blocked by low doses of NSAID

OAT/URAT - Blocked by high doses of NSAIDs
Allopurinol
reduce synthesis of Uric Acid for tx of gout

Competitively inhibits xanthine Oxidase
Febuxostat and side effects
directly blocks Xanthine Oxidase in order to reduce amounts of Uric Acid to prevent Gout

Side Effects: Diarrhea, nausea, vomiting
chemo drugs usually treat?
but cannot treat?
they treat sarcomas but can not treat lung cancer
used to save bone marrow when treating with chemo
Granulocyte colony-stimulating factor (G-CSF)

Granulocyte/Macrophage colony-stimulating Factor (GM-CSF)

Erythropoetin
Saves Kidney from Chemo therapy
Allopurinol
cell cycle phase attacked by most cell cycle drugs
G1 or S phase
easy to treat with chemotherapy because of the high mitotic index
Burkitt lymphoma
Cell cycle specific drugs
Antimetabolites-S phase (methotrexate, 4-flurouracil)

antibiotics-G2 (bleomycin)

plant alkaloids-M phase(Vincristine, vinblastine, Paclitaxel)

podophyllian alkaloids- G2 (etoposide, teniposide)
Cell cycle non-specific drugs
act on DNA directly

Alkylating agens (cyclophosphamide, nitrosoureas, cisplatin)

antibiotics (antracyclins, plicamycin, mitomycin)
cancer caused by this 50% of time

Caused by this 33% of time
1) decreased expression of p53 - apoptotic

2) Increased expression of bcl2 - antiapoptotic
pulls drug agents out of the cell...causes and efflux and a common mechanism for resistance
P-Glycoprotein
Chemotheraputic agents that do not have vomiting (3)
Bleomycin, steroids, antimetabolites
Chemotheraputic agent that causes bad vomiting
Cisplatin
chemotheraputic agent that causes severe GI complications
Anti-metabolites
Chemotheraputic agent tht causes pulmonary fibrosis
Bleomycins
Chemotheraputic agent that causes delayed leukemias
Alkylating agents
binds to guanine of DNA
Mechlorethamine ( alkylating chemo agent)
Mechlorethamine
highly electrophilic, take IV with a short half life. and can bind intrastrand or interstrand
Pathway for cyclophosphamide
Prodrug activated by cytochrom P450 to aldosphosphamide and then to phophoramide mustard which is good
Bad version of cyclophosphamide breakdown
Acrolein which causes hemorrhagic cystitis and bladder cancer
Too much of this enzyme turns cyclophosphamide into a bad version
aldehyde dehydrogenase
Side effects of cyclophosphamide
GI problems, Alopecia, but has less vomiting and less bone marror effect and spares platlets
Do not take alkylating agents with this agent because it reduces its effect
glutathiones (used for OD)
Alkylating agent that does not cause alopecia
Melphalan
alkylating agent that causes secondary leukemia
chlorambucil
take allopurinol with this alkylating agent to reduce its nephrotoxic effects
Busulfan
alkylating agents that cross the BB and god for CNS tumors
Procarbazine and Dacarbazine
alkylating agents that are MAOI so do not take them with anti-depressants
Procarbazine and dacarbazine
suffix for nitrosureas
-mustine or -ocin
used for brain cancer:
Side effects:
Notrosoureas (carmustine, Lomustine, Semustine)

Long delay of bone marrow recovery. Cross BBB so bad for nausea
Nitrosureas that do not have problem with bone marrow

Side effects:
Streptozocin and Chlorozotocin

Cause anemia
Nitrosureas with less nausea problems
Chlorozotocin
Tx pancreatic tumors
Nitrosurease: Streptozocin and Chlorozotocin
Cisplatin/Carboplatin
Cancer agent (platinum) tbat is used for epitheila tumors like ovarian, testicular, lung cancers.

cause anaphylaxis, reversible neuropathy, irreversible hearing loss, nephrotocitiy, and severe nausea
Cancer agent that causes irreversible tinnitus (hearing loss)
Cisplatin/carboplatin
antimetabolite that acts liek folic acid
Methotrexate
Affects synthesis of DNA in the S phase
Methotrexate
Do not take this cancer drug with NSAIDs
Methotreaxate
blocks Dihydrofolate Reductase thereby inhibiting DNA synthesis on cancer cells
Methotrexate
Blocks thymidylate synthetase thereby inhibiting DNA synthesis on Cancer cells
Flurouracil
used as a rescue therapy with methotrexate
leucovorin
pyrimidine analog to treat Leukemia
Cytarabine
Flurouracil/floxuridine
Pyrimide analog that inhibits thymidylate snthetase and used to stop dna synthesis in cancer patients. you use LEUCOVORIN with it for a synergistic effect.
Methotrexate Side effects
interstitial pneumonitis, nephrotoxicity, hepatic toxicity
Purine analogs
Mercaptopurine and Thioguanine
Purine analog of hypoxanthine and blocks hypoxanthine guanine phosphoriboyl transferase
mercaptourine
need to reduce dose of this purine analog if given with allopurinol
mercaptourine
used to treat leukemia
mercaptopurine
purine analog of guanine
thioguanine
thioguanine blocks what
xanthine oxidase
1)this purine analog goes through deamination first so it is ok to take it with allopurinol.

2)Versus this one which is not safe
1) thioguanine
2) mercaptourin
these Anti-metabolites inhibit DNA polymerase and afffect ribonucleotide reductase reducing CD4 levels
Fludarabine, cladribine
This anti-metabolite inhibits diphosphate reducatase
hydroxyurea
Hydroxyurea

Side effects:
inhibits diphosphate reducatse

Side effects: megaloblastic anemia, radiation recall
hapten
a molecule that by itself cannot cause an immune response but combined with something else like a protein can be immunogenic
TYPE I immune response
immediate hypersensitivity. IgE mediated and rapid. Comes in through GI, Lung and skin.

Mast cells, basophils, eosinophils

Get cross-linking and release of histamine, PGEs, Leukotriens, and cytokines
Something that is not IgE mediated response
anaphylactoid
Type II immune response
antibody-dependent cytotoxic hypersensitivity. Ab plus complement mediated lysis of cells.

IgG or IgM
Type III immune response
Immune complex mediated hypersensitivity.

IgG or IgM to get lysis or ongoing inflammation
Type IV immune response
delayed type hypersensitivity, contact sensitivity, tuberculin-type hypersensitivty

Uses Tcells

Sensitization phase - langerhans cells

Elicitation Phase - clonol expansion of Tcells in lymph nodes
Causes a Skin delayed type hypersitivity response
Toulene and Diisohydrocyonate
Innocent bystander
Type II Immune response
major determinant of a penicillin allergy
penicillin moeity
the minor determinants of a penicillin allergy
Non-enzymes like penicillenate and penicillamine
if you are allergic to penicillin you might also be allergic to?
cephalosporins and other B-lactams
Hemolytics anemia can be cuase by which immune responses?
Type II direct response (penicllin) or Type II inderect response (Bystander), or an autoimmune reaction
Agranulocytosis can be caused by?
1) Ab mediated response (type II/III)
2) when it is metabolized and effects the bone marrow
activated myeloperoxidases in neutrophiles to cause agranulocytosis
procainamide
causes thrombocytopenia
type III immune response - QUINIDINE
cause drug induced Lupus
Procainamide/hydralazine
differences between Spontaneous lupus and drug induced lupus
Drug induced has less pronounced renal effects and is only of the ssDNA sort
Aspirin-induced Asthma
not IgE response so it is an anaphylactiod response. has an upper airway response on the nasal polyps. have an allergic response to the inhibition of cyclooxygenase.
Type of diabetes prone to keotacidosis
Type 1 Diabetes
aim of treatment for both type 1 and type 2 diabetes
Fine Glycemic Control
Insulin
synthesized from pro-insulin by endopeptidases. complexed to zinc in a 6:2 ratio
these stimulate the release of Insulin
Vagal stimulation, glucagons, GH, ACTH, Beta-2 receptors

Also glucose, amino acids, fat
Inhibits release of insulin
Serotonin, hypoxia, alpha-2 receptors
Greatest stimulater of insulin release
ORAL GLUCOSE because when u take sugar orally it causes release of Gastric inhibitory protein (GIP) and secretin
how glucose signals for insulin release
It enters the beta cell, changes ATP:ADP ratio which inhibits ATP sensitive K challels and opens Ca channels which stimulates insulin release

Does this through tyrosine kinase and posphotidylinositol-3 kinase.
principal action of insulin
energy utilization and the net synthesis of carbohydrate protein and fat
where is glucose uptake not mediated by insulin levels?
Brain, Kidney tubules, Intestinal Mucosa, RBCs, Beta-cells of the islets
type of insulin compatable with all other insulin types is also the only one that can be administed through IV
regular insulin
if you have ketoacidosis then you should look out for this electrolyte loss...
K loss so if you give insulin it can reduce K+ even more
rapid acting insulin preparations
Insulin lispro, and insulin aspart
Short acting insulin preparation
regular insulin
intermediate insulin preparation
lente and NPH(neutral protamine Hagedorn)
Long-acting insulin preparation
Ultralente and insulin Glargine
the lente insulin preparations and their lengths
Short - semilente
medium - lente
long - ultralente
do not take insulin with this because it may mask the effects of hypoglycemia
beta blockers
Side effect of insulin that can be treated and what is it treated with
Insulin edema

TX: thiazide diuretic
Contraindicated in type 1 diabetes
Sulfonylureas (1st gen tolbutamide, chlorpropamide, tolazamide)
(more potent 2nd gen glyburide, glipizide, glimepiride)
1st gen sulfonoureas
(Tolbutamide, Tolazamide, Chlorpropamide)
inhibit ATP sensitive K+ channels in Beta Cells

Used for treatment of Type II diabetes mellitus.

Contraindicated in Type I and kidney insufficiencues
diabetic drug that is an antidiuretic by increasing ADH release
1st gen sulfonyurea - chlorpropamide
antaganistic effect on sulfonureas
sulfonureas are used for diabetics. Do not take with diazoxide, thiazide diuretics or ethanol
agents that might increase effects of Sulfonureas
dicoumarol, salicylates, phenylbutazine
This agent decreases the kidney excretion of sulfonureas
Probenecid
sensitive to ATP K+ channels associated with diabetes
Meglitinides (REPAGLINIDE)
these are glucose dependent in order to work their release of insulin
repaglinide
these inhibit ATP-sensitive K channels
natiglinide
Diabetic good for types II who have RESISTANCE to insulin
Metformin which is a biguanide.
do not give metformin to people with?
anyone with a condiction of hypoperfusion because they can develop LACTIC ACIDOSIS
insulin sensitizers used to help diabetes (2)
thiazolidinediones (rosiglitazone and pioglitazone)
rosiglitazone and pioglitazone
activated receptos called PPAR-y which is highly expressed in adipose tissue and do not cause them to release their free fatty acids.

do not cause hypoglycemia
acarbose
inhibits alpha-glucosidase on interstitial epithelium to delay their absorption in the GI tract

Contraindicated in any bowel disease
miglitol
inhibits alpha-glucosidase on interstitial epithelium to delay their absorption in the GI tract

Contraindicated in any bowel disease
Amylin
an islet amyloid polypeptide which is secreted with insulin. It slows gastric emptying and inhibits glucagon as well as promoting satiety
Thype of amylin that has a short duration and can be combined with insulin, metphormin, and sulfonoureas
pramlintide
Incretin, secreting, GIP
GI harmone that increases insulin release.
exenatide
a type of incretin that is a GLP-1 in order to increase insulin release
sitagliptin
inhibits dipeplidy peptidase 4 which degrades amylins and incretin so take it to increase those amounts
take this to amplify any incretins or amylins by inhibiting that which degrades them
Sitaglyptin
polypeptides
Human GH and prolactin. These things Change in the nucleus and use the JAK STAT pathway
Glycoprotein hormones
LH, FSH, TSH and hCG

2 subunits
activate Gcoupled proteins to increase cAMP and Ca++
V1 receptor of Vasopressin
involved in vasoconstriction
V2 receptor of Vasopressin
involved in anti-duretic effects as well as pro-coagulant effects (increases vWF)
Desmopressin
a V2 agonist where you do not have to worry about high BP because it is an anti-diuretic
Use low doses of desmopressing to
fix diabetes insipidus in children and those with bedwetting
use high doses of desmopressin in those with
hemophillia A or vWF disease
desmopressin overdose leads to
hyponitremia
use vasopressin to treat
diabetes insipidus, and works more on V1 receptors. OD could be hypertensive crisis
Oxytocin
Side effects:
milk ejection reflex and rhythmic contractions of uterus

Side Effects: hemorrhage and increases in BP
has a lactogenic effect like prolactin
Growth harmone
Method of action for GH
increases IGF-1 mostly in the liver
Somatostatin (GH)
has some diabetogenic effects causing a decrease in glucose uptake and increased lipolysis

Fixes turners syndrone and treats short stature.

Use with an aromatase inhibitor in order to prolong the amount of time before the epiphyseal plates close
GH receptor anatagonist
pegvisomant used for acromegaly
FSH
primarily used for oocyte or follicular MATURATION during reproductive therapy and stimulates spermatogenia for males with low sperm levels. also used to induce estrogen synthase to produce estradiol
LH
induces ovulation of ripe follicles and leutalization of granulosa cells to form a copus luteim that produces progesterone in response to LH. In males produces testosterone
differences between FSH and LH
FSH - Follicle maturation, and estrogen synthesis

LH - Follicle ovulation and progesterone/testosterone release
human Menopausal Gonadotropin (hMG) and type of it
LH and FSH mix but mainly used for FSH effects

UROFOLLITROPIN
Human Chorionic Gonadotrop (hCG)
used for its LH effects and to induce ovulation
Used for cryptorchidism (undropped testies)
hCG
adverse effects of over GnRH
too much will cause a desensitization that impairs FSH and LH release leading to a chemical CASTRATION
GnRH
used for infertility due to hypothalamic dysfunction in women without the multiple birth hyperstimulation with the FSH and LH analogs
leuprolide/nafarelin
super-agonist of GnRH. Take advantage of overstimulat of GnRH to inhibit LH and FSH. Used for management of sex hormone therapy as a PALLATIVE care (help quality of life) for things liek prostate cancer and breast cancer.

Side effects include the chemical castration
Ganirelix, cetrorelix
GnRH ANTAGONISTS. Faster induction fo chemical castration
Octreotide
novel synthetic somatostatin analog which inhibit GH release.

TX: acromegaly, carcinoid syndrome, WDHA(watery diarrhea, hypokalemia, achlorhydria
Somatostatin
inhibit GH, TSH, glucagons and insulin.
Treats WDHA and Carcinoid syndrone pallatively
sOMATOSTATIN ANALOG USED to inhibit GH release - OCTREOTIDE
Bromocriptine and cabergoline
D2 agonists used to inhibit prolactin release.

Also used for parkinsons.

adverse effects: nausea and vomiting
estrogens and progesterones produce their major affects by
effecting the nuclear hormone receptors
causing CHROMATIN REMODELING
binding to level C means
highly conserved DNA-binding
required for endometrial development
Progestins and estrogens
estrogen effect on pituitary
has both a negative and positive feedback effect
mid cycle surge of estrogen on hypothalamus
FSH/LH spike for ovulation (POSITIVE FEEDBACK)
Negative feedback of estrogen
on post menapausal women to reduce FSH and LH levels
other metabolic effects of estrogen
increase in production of clotting factors and also decreases in production of plasminogen-activator inhibitor

GIVES RISK OF THROMBOEMBOLISM
High risk of thromboembolism
estrogen in post-menapausal women because it is dose dependent
half-life of estrogen
less than 30 minutes because of its rapid hepatic metabolism
adding an alkyl group to estrogen
makes ethinyl estradiol which has a much longert half life and resist hepatic first pass metabolism for use with once a day treatment
esterfiing the estrogen at the 17 position
estradiol cypionate and estradiol valerate

the molecule is now more hydrophobic. So you do not want to give it orally...so give it IM. This is good for long lasting estrogen to induce pubertal changes
analogs of estrogen esterfied but for testosterone
testosterone enanthate and testosterona cypionate which last long
testosterone propionate
less dose required
this is unique to estrogens and required for activity
the aromatic first ring
estrone sulfate/equilin sulfate
a conjugated estrogen. absorbed in LOWER GI tract. used in ORAL hormone replacement therapy of POST menapausal women. LESS POTENT THAN SYNTHETIC ETHINYL ESTRADIOL
used as a oral contraceptive most popularly
ethinyl estradiol which has a 17-alkyl constituent
mestranol
another potent estrogen that is used for oral contraceptives but it isa progrugnorethindrone
classic progestin used as an oral contraceptive

and its problesm
northindrone which can cause troublesome of beneficial effects

have weak androgenic effects and anti-estrogenic effects
19-notestosteron derivatives that have minimal androgenic or estrogenic effects
desogestrel and norgestimate
reason for combining estrogen and progestin for contraceptives
then u can use lower dose of estrogen and u get a predicatable onset of menses and the least chance of fertility impairment
have a lower dose of estrogen but they are not good for ladies who want kids in the future
mini-pills which are progestin alone
best contraeptives for those who want future kids
combination pills
depot injection of medroxyprogesteron acetate
depoprovera which is an oral contraceptive
side effect of these oral contraceptives include increased risk of breast cancer in post-menopausel women
progestins
side effects of these oral contraceptives are nausea, cholecystits and darker complexion on what aged women?
ESTROGENS
PRE-MENAPAUSAL
severe side effects of estrogen
Venous thromboembolic disease and some uterine cancers which will not be caused by progestins
sever side effects of combination oral contraceptives
myocardial infarction and stroke. Also in post menapausal women you get BREAST CANCER
give this for advanced prostate cancer
Estrogens - diethylstilbestrol
tx: for hereditary angioneurotic edema and the side efects of taking this drug
DANAZOL

S.E.: benign hepatic tumors
flutamide
non-steroidal antagonist of androgen receptor that prevent flare reaction associated with GnRH super agonist analogs
bicalutamide
non-steroidal antagonist of androgen receptor that prevent flare reaction associated with GnRH super agonist analogs
androgen receptor agonist used to treat hirsuitism in women
spironolactone
makes androgens less potent by inhibits 5-a reductase which converst testosterone to dihydrotestosterone
finasteride
use this to tx benign prostatic hypertrophy
finasteride
tamoxifen
a selective estrogen receptor modulator which acts like an antagonist on breast tissue but an agonist on bone and uterus

TX: BREAST CANCER

SE: thromboembolism, uterine cancer
Raloxifene
Seective estrogen receptor modulator. Agonist on some parts, and antagonist on other parts. This one is used for OSTEOPEROSIS

increased risk of thromboembolism
Clomiphene
Seective estrogen receptor modulator. Agonist on bone and antagonist on breast.

tx: infertility
Best things to use for breast cancers
Aromatase inhibitors - anastrazole
Main endogenous glucocorticoid in the body and its purpose
involved in regulation of internal metabolism

CORTISOL
Main mineralcorticoid
Aldosteron involved in salt water homeostasis
where are steroids made?
adrenal cortex
made in zona glomerulosa
aldosterone
zona fasiculata
cortisol
zona reticularis
sex steroids
main sex steroid and the enzyme necessary for it
dihydroepiandrosterone P450
Apposite of transcortin
Albumin which has low affinity and high capacity binding. as oppossed to transcortin (corticosteroid-binding globulin) which has high affinity and low capacity binding
which is more widly distributed...Glucocorticoid receptors or mineral corticoid receptors?
glucocorticoid receptors
glucocorticoids can bind to which receptors
glucocorticoid receptors or mineralcorticoid receptors
Cortisol binds to which receptors? How do you change it?
because it is a glucocorticoid it binds to both glucocorticoid and mineralcorticoid receptors. However if you convert it to cortisone it only binds to glucocorticoid receptors
11B-hydroxysteroid dehydrogenase
this converts cortisol to cortison so it can only bind to glucocorticoid receptors instead of both gluco and mineral

You get a mineralcorticoid excess when this enzyme is messed up as in a genetic insufficiency or eating black licorice
glucocorticoids side effects
want to INCREASE levels of glucose so can cause diabetogonic effects
Aldosterone
mineralcorticoid that increase ENaC channels to increase sodium reabsorption
increase in sodium levels caused by aldosterone can lead to
atherosclerosis, stroke, hypertension
glucocorticoids do what to prostiglandins?
they decrease them thereby getting an ELEVATION OF BP
hydrocortisone can be taken?
orally or IV right into the joints
cortison negative feedback loop
effects the hypothalamus and pituitary in order to inhibit productions of cytokines like IL1/2/6 and TNF-a to stop an acute organ rejection
why would you give hydrocortison IV
because then the 11-b hydroxysteroid cnt convert it to cortisone and it can be used to activate mineralcorticoid receptors in the case that someone has hypotension - acute insufficiency of aldosterone
a type of chronic adrenal insufficiency
addisons disease
TX for addissons disease
it is a chronic adrenal insufficiency. You want to give somethign to increase the levels of mineralcorticoids instead of glucocorticoids so give FLUDROCORTISONE
congenital adrenal hyperplasia
can be when the 21beta-hydroxylase enzyme is missing so cortisol can not do negative feedback because it is not created and thus increased ACTH and increased sex hormones
Cushings syndrome
instance of producing more cortisol regardless of function. can be due to ACTH or anything
Cushings Disease
Tumor in the pituitary that causes an excess of ACTH which increases Cortisol levels
how to distinguish between cushings syndrome and disease
Dexamethasone suppression test - if the levels are supressed you have cushing DISEASE
excessive levels of cotrisol by drugs or by cushings can lead to:
osteroperosis and cataracts.
mitotane
- of adrenocortical steroids
ONLY DIRECT CYTOTOXIC EFFECT to kill cells int he adrenal cortex.
aminoglutethimide
inhibitor of adrenocortical steroids
blocks the CYP450 or 11B-hydroxylase in order to inhibit levels of cortisol in cushings syndrome
Ketoconazole
inhibitor of adrenocortical steroids

used as an antifungal but in high doses can block the 17hydroxylase enzyme which blocks pregnenolone to 17 hydroxypregnenelone which is used to make cortisol. This does NOT affect the aldosterone pathway so it is te BEST for Cushings DISEASE
Trilostane
inhibitor of adrenocortical steroids

inhibits the 3B dehydrogenase to treat cushings syndrome
metyrapone
inhibitor of adrenocortical steroids

inhibits 11B-hydroxylase but is not as good as the rest to stop production of aldosterone or cortisol
restictive lung disease
reduction in lung volumes with a normal FEV1/FVC ratio
obstructive lung disease
reduction in expiratory flow rates manifested by a reduced FEV1 and FEV1/FVC ratio
what we use to measure airway hyperresponsiveness (asthma)
Methacholine challenge test...If FEV1 drops 20% it is considered a hyperresponsive effect
T cell associated with delayed type hypersenesitive
TH1, more the people who have been exposed to things in the past (3rd world)
T-cell associated with allergic inflammation
TH2, westerners who have all these allergies
Short (fast) acting beta-2 agonists (3)
albuterol, metaproterenol, terbutaline

These are used to help with asthma. they are good for rescue
Albuterol
a Beta 2 agonist that can cause rapid bronchodilation in those who have asthma. But can develop tolerance quickly and inhalation is the best route with teh least side effects
Long-acting beta-2 agonists (2)
come from epinephrine and isoproterenol. They are SALMETEROL AND FORMOTEROL

Used for asthma but are not as effective against the inflammation as the short acting. Plus these ones are more life threatening
Beta Agonist side effects
cardiac problems, tremor, hypokalemia, and HYPOXEMIA - give oxygen to those patients
Levelbuterol
used for asthma and it is more specific because it has the R isomer instead of the S isomer which is less effective
theophylline

S.E.
a bronchodilater that is an antagonist of adenosine.Has anti-inflammatroy effects and also suprresses permeability edema and is ONLY AVAILABLE ORALLY

S.E. LIVER PROBLEM
aminophylline
a type of theophylline used for asthma but it is not pure but can be given IV
theophylline efects P450 and increases the levels of these drugs (5)
cimetidine, erthromycin, ciprofloxicin, allopurinol, propranolol
both theophylline and beta agonists stimulate...
cAMP
Most effective in COPD
Ipratropium Bromide (Atrovan) which is an anti-cholinergic
Ipratropim Bromide, tiatropium
Atrovan. It is a non selective anti-cholinergic agentwith a slow duration fo action and used to reverse bronchoconstriction to help asthma and COPD
Atropine
An anticholinergic but is not used as much because it is a tertiary ammonum and rapidly absobered if used for asthma to cause tachycardia
why do you use ipratropium Bromide to help with asthma instead of Atropine if both are anti-cholinergics?
Ipratropium Bromide is a quarternary ammonia as oppossed to teh tertiary atropine so it is less absorbed and has less adverse effects
most potent anti-inflammatory agents
corticosteroids
if you are giving some1 with status asthmaticus beta agonists, what else should u give to make them more responsive?
glucocorticoids such as methyl-prednisolone
method of administration for corticosteroids for use with asthma
inhaled or topical because they have less side effects than when given orally
corticosteroids used for asthma (6)

S.E.
Beclomethasone, triamcinolone, diflusinide, flucticasone, budesonide, mometasone fluroate

local side effects like oral thrush, dysphnoia and worsened asthma
problem with corticosteroids in asthma (not side effects)
they have a delayed effect so do not use them for rescue therapy
Side effects of taking oral corticosteroids
adrenal suppression, cataracts, hip necrosis, glucose intolerance
Side effects of inhaled corticosteroids
mostly local, coughing, oral thrust, weight gain, osteoperosis
anti-leukotrien used for asthma (3) in patients who have ASPIRIN SENSITIVITY
montelukast and only needs to be taken once a day

Safirlukast, zileutin need to be taken several times a day and are more dangerous
Cromolyn
used against asthma. is a prophylactic insoluble salt.

It STABILIZES mast cell degranulation and work better on young adults. It is specific for IfE and mast cells.

Pre-treat with this and you block both DELAYED AND IMMEDIATE REACTIONS

side effects of hoarseness and sore throat
Nedocromil
used against asthma. is a prophylactic insoluble salt.

It STABILIZES mast cell degranulation and work better on young adults. It is specific for IfE and mast cells.

Pre-treat with this and you block both DELAYED AND IMMEDIATE REACTIONS

side effects of hoarseness and sore throat
Omalizumab
monoclonal antibodies used to help astma. an IgG monoclonal antibody, for anti-IgE. not anaphylactogonic and decreases free IgE

Taken SUBCUTANEOUSLY
Infleximab
a monoclonal antibody that is used for astma becuse it TBF-a reducer
Which thyroid hormone is more avidly bound and thus has a longer 1/2 life
T4
which thyroid hormone is moreactive?
T3
deficiency of thyroid hormone in fetus is
creatinism
hypothyroidism is associated with
HASHIMOTOS THYROIDITIS

hypercholesterolemia and cold intolerance and myxedema coma.

Can treat with replacement therapy of T4 which is levothyroxine
Levothyroxine
analog of T4 and used to treat hypothyroidism associated with hashimotos thyrdoiditis
liothyronine
analog of T3 and used in more serious hypothyroidism associated with myxedema coma
usual cause of hyperthyroidism
graves disease which stimulates TSH and constant stimulation of thyroid hormone synthesis and secretion
tx: for hyperthyroidism/graves
the thiourea deriviatives: propylthiouracil and methimazole.

they INHIBIT THYROID PEROXIDASE
Which thiourea derivat do you give ina preagnant woman?
propylthiouracil because it doesnt cross the placenta as well as methimazole
this thiourea derivated also inhibits 5'-deiodinase as well as thyroid peroxidase
propylthiouracil. By inhibiting this enzyme it stops the conversion of T4 to T3
which thiourea is more potent?
methimazole is more potent than propylthiouracil
side effects of methimazole and propylthiouracil which are thiourea
agranulocytises
high-dose iodide
effects take place in 24 hours. it inhibits the release of TSH so you have less thyroid hormone being released

USED FOR THYROID STORM.
radioactive iodide
corrects hyperthyroidism. allows u to kill thyroid without affecting parahtyroid.
most likely cause of heavy metal toxicity
lead
other likely causes of heavy metal toxicity (3)
arsenic, iron, mercury
ligands suceptible to heavy metals usually include
sulfhydryl groups
chelating agents
used against hte heavy metal poisenin
which is more difficult to detect? acute or chronic metal toxicity?
chronic
all inorganic forms of heavy metals cause
GI Toxicity leading to nausea, vomiting, abdominal pain, diarrhea, MULTI-ORGAN toxicity,
all heavy metals cause nephrotoxicity EXCEPT?
Iron
chelating agents dnt hit this part of the body and thus they are ineffective for treatment of?
They dnt hit the CNS and ineffective for tx: of organic forms of tetrahydral lead or methyl mercury
chelating therapy is most useful for?
acute metal toxicity associated with high blood metal levels
most common form of lead poisoning
environmental on children
lead effects which steps of heme synthesis?
o-aminolevulinic acid dehydrogenase and ferrochelatase leading to an anemia
blood level of lead to be problem
>10
percentage of homes where kids are living that are made before 1950 that require lead screening
>27% of homes
if an ADULT has symptoms of lead poisoning or encephalopathy or their pB>100 give them what chelating therapy?
dimercaprol + CaNa2EDTA
If a Child has encephalopathy of is symptomatic with a pb>70
give them dimercaprol + CaNa2EDTA
if an adult has mild syptoms of pb70-100 or a child has mild symptoms with a pb of 45-69 then give?
give succimer
dimercaprol
a dithiol used IM which is used for acute lead toxicity with CaNa2-EDTA. it lowers lead levels in CNS. It is also a single agent treatment for arsenic toxicity or mercury
Single agent treatment for ACUTE arsenic poisoning
Dimercaprol
Single Agent treatment for Acute mercury Toxicity
Dimercaprol
CaNa2-EDTA
used for lead poisoning in conjuction with dimercaprol. However it has a higher affinity for lead and helps better with its excretion. It also helps it to be removed from the bone.
good oral analog of dimercaprol
succimer
single agent treatment for MILD toxicity of lead poisining at levels of 45-60
succimer
single afent therapy for mild arsenic or mercury poisoning
succimer
penicillamine
used to treat copper poisonnign or prevent copper accumulation in wilsons disease
deferoxamine
used to treat iron poisoning
prussian blue (ferric hexacyanoferrate)
chelating agent with high affinty for cesium and thallium. NOT ABSORBED ORALLY. TX: radioactive bombs and thallium poisoning