Pharmacology Unit 4

lipid

hypolipidemic drugs are meant to help decrease — levels in blood

atherosclerosis, LDL, macrophages

—: plaques build up in arterial walls in response to damage/inflammation, — migrates to the injured area and is oxidized, (prev) and damage causes — to be recruited

foam

when macrophages attempt to phagocytose LDL they convert into — cells

plaques

oxidized LDL and foam cells form the basis of — → atherosclerosis

triglycerides

LDL, HDL, VLDL provide a way for — to move through the body

lipoprotein

makes up LDL, VLDL, HDL is used to transport cholesterol and apoprotein

chylomicron

is similar to lipoproteins, responsible for triglyceride transport, is made/absorbed from the intestines

small intestine, lymph

chylomicrons are absorbed in the — — and then are absorbed by the — which is drained into the blood stream

liver

while some cholesterol is absorbed in food, most cholesterol is synthesized in the —

blood vessels

LDL and VLDL bring cholesterol to the — —

empty, plaques

HDL is — and released by liver to pick up cholesterol/lipids from blood or — and bring it back to the liver

energy

triglycerides from the blood are lipids that provide an — source for the body

HMG-CoA reductase inhibitors, cholesterol absorption inhibitors, bile acid sequestrants, PCSK9 inhibitors

what are the 4 classes of hypolipidemic drugs?

HMG-CoA reductase, cholesterol, LDL/VLDL, HDL, intestinal, rhabdomyolysis, liver

atorvastatin is a — — inhibitor (statin) hypolipidemic drug

MOA: decreases — synthesis by inhibiting (<prev), this causes a decrease of —/— synthesis and an increased expression of LDL receptors, and an increased production of —, this also causes decreased inflammation

Adverse effects: insomnia, — cramps, — (death of skeletal muscle via nicrosis)

Contraindications: — disease, pregnancy

cholesterol absorption, NPC1L1, metabolized, liver, abdominal pain, myalgia

ezetimibe is an — — inhibitor

MOA: blocks — on brush border of intestines, decreasing cholesterol absorption in the intestines, drug is — in the intestinal wall and recirculates between — and intestines

Adverse effects: — —, fatigue, — (muscle pain)

bile acid, resin, insoluble, cholesterol, obstruction

Cholestyramine is a — — sequestrant hypolipidemic drug

MOA: is an ion exchange —, binds to form — complex with bile acids, blocking the reabsorption of bile salts containing —

adverse effects: constipation, intestinal —

charged, exchanged

ion exchange resins have a — functional group that can be lost or —with another functional group

PCSK-9

helps with homeostasis, internalized and breaks down LDL receptors, prevents cells from taking up too much cholesterol

PCSK-9, antibody, adjunct, hepatocyte, back, bruising

alirocumab is a — inhibitor that is a hypolipidemic drug

MOA: it is an — that targets (<prev) preventing it from binding to LDL receptors

alirocumab is an — therapy, it increases LDLR expression on —

Adverse effects: cold/flu-like symptoms, — pain, — at injection site

aspirin, vitamins, cholesterol

bile acid sequestrant drug interactions: drug such as —, penicillin, and — can bind to resins, preventing them from binding to —, so you want to make sure to take resins ~ an hour before these other drugs

CYP384, increased, propranolol

Drug interactions for statins: the body relies on — to metabolize statins, drugs or food could block the activity of (prev) causing — statin levels in the blood leading to an increased chance of toxicity

— may help to decrease some statin effects

GLP-1 agonist, insulin, structurally, AA, hypoglycemia, thyroid

Semaglutide is a — — that is a hypolipidemic drug

MOA: acts as an agonist on GLP-1 receptors which is highly expressed in the pancreas and throughout body, increases — sensitivity, it is — similar to GLP-1 by some — substitutions increase its half-life

decreases GI motility and appetite encouraging fat cell metabolism

Adverse effects: —, tachycardia, — tumors/cancer

gastric secretions

all the stuff the stomach makes and pumps out (primarily HCl)

bacteria

HCl is protective against — and breaks down food

pepsin

enzyme that is activated by HCl to digest proteins

G cells

— —: in pyloric gland, signals cells in gastric gland to make gastrin in response to changes in pH of stomach

Chief cells

— — in the gastric gland, make pepsinogen (inactive version of pepsin)

parietal cells

— — in gastric gland, produces HCl

ACH, gastrin, histamine, pH

there are 3 signals that parietal cells receive to indicate the need for HCl release: — (released by the parasympathetic system), — (released from G cells and pancreas), — (binds to parietal cells H2 receptors, is released in response to increased — or stomach stretching)

aquaporin, ATPase, bicarbonate/chloride exchanger, HCl

CO2 and H2O enters the parietal cells through the — channels which produces bicarbonate and a hydrogen ion, the H+ leaves the cell into the stomach lumen via the H+/K+ —, Cl- enters and HCO3- exits the cell via the —/— —, Cl- leaves the cell into the stomach lumen giving the stomach both the the parts for —

peptic, HCl, nausea, heartburn

— ulcers are ulcers that form in the stomach or intestines due to damage to the mucus membrane (that is meant to protect organs from —) → damage to stomach/intestinal cells

overtime they cause periodic pain, —, loss of appetite, —

HCl, H. pylori, NSAIDs, prostaglandins

causes of peptic ulcers: overproduction of —, stress, — — infections (either too much or in combination with something that decreases the mucus membrane), — (decrease — [which help to make mucus layer])

GERD, LES, CT, hiatal hernia, esophageal, precancerous

—

symptoms: chronic heart burn, chronically

Cause: — relaxes at inappropriate times causing acid reflux in the esophagus

associated issues: — disorders, delayed stomach emptying, pregnancy, — —, smoking

when left untreated it can cause: — inflammation/ulcers, narrowing of the esophageal, — changes

acid, mucosal

treatment goals for ulcers: decrease — production and increase — barrier

acid, erosion

treatment goals for GERD: decrease — production and prevent —

antibiotics

ulcers caused by H. pylori also needs to be treated with —

caffeine, alcohol, NSAID

Lifestyle factors that can help decrease GERD and ulcers include: smoking cessation, reducing/eliminate — and —, eliminate — if possible and reduce stress

H+/K+, Zollinger-Ellison, infections, diazepam, phenytoin

omeprazole is a proton pump inhibitor (PPIs)

MOA: inhibits —/— ATPase pump

Is used to treat ulcers, GERD, or — — syndrome

Adverse effects: headache, GI disturbances, long-term use may increase risk of —

Drug interactions: it can increase plasma levels of — and —

antagonist, HCl, constipation

Famotidine is used treat ulcers and GERD, less potent than PPIs

MOA: — H2 receptors (prevents histamine from binding) → decreased — and pepsin release

adverse effects: headache and —

prokinetic, LES, antiemetic, tardive dyskinesia, epilepsy, ESP

metoclopramide is a — drug

MOA: stimulates contractions in —

treats GERD and — (vomiting)

Adverse effects: nausea, — — after long-term use, tachycardia

Contraindicated in —

drug interactions: has an additive effect with drugs that cause —

ductless glands

the endocrine is a collection of disconnected — —

target, longer

hormones bind to receptors on — organs have a slower onset of action and a — duration on the body than the nervous system

activate, expression

MOAs of hormones:1. — certain enzymes that cause a chemical reaction

2.influence gene — by causing an increase or decrease of synthesis of certain protein

lipid soluble

— — hormones can diffuse through the cell membrane and activate receptors in the cytoplasm

water

— soluble hormones primarily activate receptors embedded in the cell membrane →activation of enzymes

master

the pituitary gland is the — gland

hypothalamus

the — controls the pituitary

tropic

the anterior pituitary releases — hormones that bind to organs and cause release of other hormones

kinases protein

hypothalamus produces hormones and delivers them to the pituitary gland via — — transport

FSH, LH

GnRH from the hypothalamus causes — and — to be released from the pituitary

estrogens

— act on hypothalamus and pituitary as a negative feedback

LH

after estrogens peak there is an — surge that causes ovulation

corpus luteum

during ovulation the follicle releases the egg that causes the — — to be left behind which produces progesterone

endometrium

progesterone helps to prepare the — for the baby

hCG

— determines “what happens next”, primarily produced by the embryo

corpus luteum, decrease

if the embryo doesn’t produce hCG levels then the — — degrades and there is a — of progesterone and estrogen levels

estrogen, hot flashes, density, concentrate

menopause/surgically-induced menopause causes severe — decreases which can cause vasomotor symptoms (such as — —), decreases in bone —, insomnia, irritability, inability to —

osteoblasts

estrogen increases the life-span of —/bone formation

replacement therapy, depression, thromboembolism, reoccurance

estradiol is a — — used to treat menopause

it is essentially estrogen

can be taken via oral, transdermal, IM options

Side effects: nausea, vomiting, —

Toxic effects: increased risk of —, stroke, breast cancer —

anovulation

when ovaries do not release an egg

PCOS, hypothalamus

factors causing anovulation: —, obesity, low body weight, — disease, hyperprolactinemia

fertility, ovulation, antagonizes, hyperstimulation

clomiphene is a — drug that stimulates —

MOA: SERM that — estrogen receptors in the hypothalamus

Adverse effects: hot flashes, nausea, — (an ovary releases and egg every cycle)

happened, estrogen, progesterone, ovulation

oral contraceptives trick the body into thinking ovulation has —

typically made of combination — and — pills

Goal: to prevent —

monophasic, nausea, cardiovascular

Loestrin is a — oral contraception drug

Side effects: —, vomiting, depression

Toxic effects: — effects also seen in replacement therapy

monophasic

fixed amount of hormones in every oral contraceptive pill

multiphasic

doses of hormones vary across the cycle in the oral contraceptives

regular

emergency contraceptives are not for — use

progesterone, LH, motility, vomiting

Levonorgestrel (Plan B) is a — receptor agonist

MOA: 1. delays ovulation by pushing off — surge and killing the sperm

2 decreases sperm —, may influence implantation (data is inconclusive)

Side effects: nausea, —, depression

confirmed

the abortion pills are used when there is a — pregnancy

combo

mifepristone and misoprostol are — abortion treatments

antagonist, thins, detachment, heavy bleeding, abdominal

Mifepristone is an abortion pill

MOA: PR —, it — the endometrium and causes embryo —

Adverse Effects: fever, — —, — pain (labor level)

prostaglandin, labor, heavy bleeding, abdominal, teratogen

misoprostol is an abortion pill

MOA: synthetic —, encourages — contractions

Adverse effects: fever, — —, — pain, known — of the baby survives

cushing’s, cortisol, competes

mifepristone is also used to treat — syndrome which is caused by elevated — that leads to diabetes

MOA: — with cortisol

induce, HCl

misoprostol is used to help — labor in a hospital setting, can also be used to treat ulcers because it inhibits — production

testosterone, ABP, secondary, anabolic

in males, LH causes — release and FSH causes — release

this results in male developments, — sex developments, — effects

androgen, steroid, transcription, deficiency, hypogonadism

testosterone is given in — replacement therapy

MOA: testosterone binds to — receptors to promote gene —

Primary indication: androgen —, — (reduced or no sex hormones)

testes

primary hypogonadism is when there is an issue with the —

communication

secondary hypogonadism is when there is an issue with body — with gonads, pituitary or thyroid

testosterone, transcription, osteoporosis, liver

oxandrolone is used as an androgen replacement therapy

MOA: — binds to steroid receptors to promote gene —

Adverse Effects: weight gain , —, PED, shortness of breath, — issues

small, irregular, nucleotides

cancer cells typically have a — cytoplasm, an — nucleus/ multiple nuclei, and multiple —

solid

tumor type that is a mass of cells creating a lump, usually restricted to one location, but can metasize

diffuse

cancer type that is present in the blood stream (leukemia)

surgery, radiation, chemo, immunotherapy

what are the 4 main treatment approaches for cancer?

precision

— medicine is a new more personalized treatment method

specific

cancer treatments can be — to the cell cycle or not

dividing

cell cycle specific (CCS) treatments are only effective in killing actively dividing cells

irrespective

cell cycle nonspecific (CCNS) kills cell — of what they’re doing cell-cycle wise

systemic, BM, skin

chemotherapy toxicities are typically —, and can effect —, GI tract, —, hair

myelosuppression

decrease in bone marow’s ability to make myeloid cells, has a negative impact on stem cells

alkylating, CCNS, liver, covalent, cross-linking, teratogenic

cyclophosphamide is an — drug and is — (but is more effective in dividing cells)

MOA: bioactivated in —, damages DNA by forming a — bond with an alkyl group and encourages — —

cancer treatment

Adverse effects: carcinogenic, —

alkylating, platinum, CCNS, covalent, DNA, carcinogen

cisplatin is an — drug that is a — derivative, is a —

MOA: forms — bonds between alkyl groups, damages — and encourages cross-linking

cancer treatment

Adverse effects: —, teratogen

purines, pyrimidines, S

antimetabolites are drugs that are structurally similar to —, —, and folic acid, these drugs are CCS and are most effective during the — phase

antimetabolite, antagonist, purines, thymidine, dihydrofolate, myelosuppression, rash

methotrexate is an — drug that is a folic acid —

MOA: inhibits synthesis of — and —, and inhibits the activity of — reductase

Used to treat cancer

Adverse effects: —, nausea, diarrhea, —

antimetabolite, pyrimidine, CCS, thymidine, myelosuppression, vomiting

fluorouracil is an — drug that is a — antagonist, it is also a —

MOA: it inhibits synthesis of —

treats cancer

Adverse effects: —, nausea, —

plant, microtubules, disassembly, neuropathy

paclitaxel is a drug derived from — products

MOA: it binds/inactivates mitotic — allowing them to stabilize and prevents —/freezes the cytoskeleton

treats cancer

Adverse effects: myelosuppression and peripheral —

bacteria, intercalation, topoisomerase, ROS, cardiac

doxorubicin is a drug derived from —

MOA: causes DNA — (changes the shape of the helix), inhibits —, increases — levels

treats cancer

Adverse effects: myelosuppression and — disturbances

hormone, SERM, estrogen, breast, thromboembolism, endometrial

tamoxifen is a — antagonist

MOA: it is a —, used as an antagonist for — receptors in — cancer

Adverse effects: —, uterine cancer, increased risk of — cancer

hormone, analog, LH, FSH, GnRH, headaches

Leuprolide is a — antagonist,

MOA: GnRH — that (eventually) inhibits — and — release, eventually the anterior pituitary stops expressing receptors of —

treats cancer

Adverse effects:—, nausea, hot flashes

hormone, androgen, replication, hot flashes, Gi, liver

flutamide is a — antagonist

MOA: — receptor antagonist, decreases testosterone specific to DNA —

treats cancer

Adverse effects: — —, — disturbances, change in — function

antibody, EGFR, progression, immune effector, head, neck, tachycardia, breath

cetuximab is an — immunotherapy

MOA: blocks — activation → decreased cell cycle — and cell survival, recruits — — cells that will recognize the Ab on the cancer and kill it

Treats — and — cancer and colorectal cancers

Adverse effects: Lesions/rashes, —, shortness of —