Pharma Topic List A Flashcards
A.5. Local anesthetics Drugs
cocaine
lidocaine
articaine
bupivacaine
A.5 Local Anesthetics - MoA
blocks Na+ channel inhibiting AP
LA cause vasodilation add vasoconstrictor like E
Frequency dependent Blockade - affects depolarized nerves - sensory, A-delta, C - more than motor
Onset - LA with lower pKa have a quicker onset - since more drug will exist in unionized form. thereby it allows penetration into the neuron easier
A.5 Local Anesthetics - Factors Affecting half life of LA
- severe liver disease
- competition with other drugs fro the same enzyme
- decrease in hepatic blood flow
cocaine
Ester - metabolized by pseudocholinesterase
Topical
ISA - reuptake inhibiotr
DoA=1-2h
SE: - allergy, CV and CNS disturbance, coronary spasm, euphoria
A.5. Local anesthetics Drugs
lidocaine
amide - met CYP450 (CYP3A4)
Fast onset of action - short, local procedures
post-op analgesic
DoA - medium
can produce autonomic block in ischemic conditions - Class Ib antiarrythmic
Lidocaine interacts with antiepileptics
A.5. Local anesthetics Drugs
articaine
Amide
most rapid onset of action
very high potency
has an ester on its side chain - can be inactivated by hydrolysis
A.5. Local anesthetics Drugs
bupivacaine
Amide - CYP450 (CYP3A4)
Long duration of action
highest potency
high protein binding
used for long procedures
Cardiotoxic - severe myocardial depression esp if administered into blood
A.5. Local anesthetics Drugs
A.6. Glucocorticoids for oral and parenteral use - GC summary
GC-R are found through-out the body.
When they bind the GC-R complex dimerizes –> recruits coactivators or corepressors –> translocates into the nucleus, where it attaches to the GC-R gene element (GRE) –> gene expression modulation
Activation:
-Annexin1 –> dec PLA2
- enzymes for gluconeogenesis and AA metabolism
- adrenergic-R on vascular and bronchial smooth muscle
Repression:
COX2, NOS, cytokines, interleukins, cell adhesion molecules
A.6. Glucocorticoids for oral and parenteral use -Drugs
hydrocortizone
prednisolone
methylprednisolone
dexamethasone
triamcinolone
hydrocortizone
synthetic cortisol
short acting 8-12 hours
same affinity GC:MC
PO,IM, intra-art
Tx- DoC primary adrenocortical insufficiency (Addisons) or CAH - congenital adrenal hyperplasia
helps with IBD - enema
inibits peripheral conversion T4 to T3 - tx - thyroid storm
A.6. Glucocorticoids for oral and parenteral use
prednisolone
Active metabolite of prednisone
systemic steroid
PO, topical
intermediate acting 12-36 hr
GC:MC - 4 : 0.8
Tx - DoC for systemic anti-inflamm and immunosupression
inhibits cytokine gene expression
severe persistent asthma
thyrotoxicosis
A.6. Glucocorticoids for oral and parenteral use
methylprednisolone
Dose: 4 - 250mg
PO, parenteral
intermediate acting 12-36 hr
GC:MC - 5 : 0
TX - DoC for systemic anti-inflamm and immunosupression
thyrotoxicosis
IBD - PO or inj
Antiemetic in CIV
Urgent cases IV - anaphylaxis, bronchial asthma, brain edema, hepatic coma
A.6. Glucocorticoids for oral and parenteral use
dexamethasone
synthetic GC - Dexathemasone suppression test - suppresses cortical release in normal individuals but not in those with cushings
long acting 36 - 72 hours
DoC - supression of ACTH, anti-inflamm and immunosupress where water retention is unwanted
-IM mother within 48 hr premature birth to hasten fetal lung maturation
Neoplastic - dec brain edema
used in conjuction with aminogluthetimide to dec estrogen in breast cancer
A.6. Glucocorticoids for oral and parenteral use
triamcinolone
PO, Topical, parenteral
intermediate acting 12-36 hr
GC:MC - 5 : 0
Tx - allergic rhinitis spray
More Toxic than others
A.7. Mineralocorticoids. Topically applied glucocorticoids Drugs
fludrocortizone
fluocinolon
mometazone
budesonide
fluticazone
metyrapone
A.7. Mineralocorticoids. Topically applied glucocorticoids Drugs - Effect of MC
MC are steroids produced by the adrenal cortex. MC-R complex effects gene expression.
Genomic Receptor Action:
- inc Na+/K+ transcription
- inc ENaC channel activity
- inc expression of pro-fibrotic molecules
- inc NADPH expression
- inc ROS pro-inflam
Non-Genomic
- inc Na+ reabsorption
- inc K+ and H+ excretion - via collecting duct
fludrocortizone
MC
DoC for replacement therapy for adrenal hypofn
Acute/Chronic or post Adrenalectomy
PO
long duration of action
inc Na+ reabsorption in distal tubules and K+ ad H+ efflux
A.7. Mineralocorticoids. Topically applied glucocorticoids
fluocinolone
MC
TX - implanted in chronic non-infectious uveitis
ointment in derma
A.7. Mineralocorticoids. Topically applied glucocorticoids
mometazone
Topical GC - Aerosol - bronchial asthma
nasal spray - allergic rhinitis
A.7. Mineralocorticoids. Topically applied glucocorticoids
budesonide
Topical GC Aerosol - bronchial asthma
Nasal Spray - allergic rhinitis
Enema in IBD (suppository)
A.7. Mineralocorticoids. Topically applied glucocorticoids
fluticazone
Topical GC - aerosol in bronchial asthma
A.7. Mineralocorticoids. Topically applied glucocorticoids
metyrapone
Adrenocortical antagonist
inhibits beta hydroxylase - in ACTH producing tumors
used to dx test of ACTH fn
can be used to tx Cushings
A.7. Mineralocorticoids. Topically applied glucocorticoids
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity - Drugs
testosteron-undecanoate
bicalutamide
finasteride
goserelin
degarelix
sildenafil
nandrolon
testosteron-undecanoate
Synthetic steroid.
NOT PO – high first pass metabolism – transdermal patch, inject, gel.
TX- replacement tx in hypogonadism, maintain libido.
In case of PO needs to be absorbed with lipophilic vehicle into lymphatics.
SE – enhance hematocrit, excessive masculinization.
CI – prostate or breast cc. interact – may improve glucose tolerance, enhance anti-coagul in coumarins.
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
bicalutamide
androgen R antagonist, competitive inhib.
PO.
TX – metastatic prostate cc.
CI – hepatotoxicity it’s a CYP3A4 inhibitor.
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
finasteride
5-alpha-reducatse inhibitor, dec DHT which dec testosterone.
Moderately effective in dec prostate size in men with BPH.
PO.
TX – male baldness and female hirsutism.
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
goserelin
GnRH analogue.
t1/2=4h.
Continuous GnRH until there is a downregulation of the GnRH-R.
Tx – prostate cc. breast cc. severe endometriosis, IVF.
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
degarelix
GnRH antagonist.
Blocks GnRH R in the pituitary dec FSH and LH. Dec effect on Leydig cells to produce testosterone.
Tx – prostate cc. women IVF.
SE – QT prolong, heatwave, dec gluc tolerance, dec bone density
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
sildenafil
PDE5 inhibitor “Viagra”.
causes inc cGMP - vasodilation
PO.
TX – pulmonary HTN, erectile dysfn.
CI – nitrates.
SE – severe hypotension, priapism
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
nandrolon
Synthetic steroid analogue only used for anabolism, not used for hormonal purposes.
Indication – convalescence after trauma, surgery, prolonged immobilization, anemia as a consequence of renal fail.
SE – masculization women, androgen with gestagen activity – CV risk, endometrial bleeding after stopping, sodium retention, edema, elder male- prostate hyperplasia.
CI – pregnancy, prostate cc, infants, young, breast cancer males.
ABUSED in sports
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity
A.8 Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity - Sexual Activity
Sexual Activity
– Hormonal tx – testosterone-udecanoate.
Inhibitor PDE-5 – Sildenafil, tadalafil.
Intracavernous tx used for tx or for dx of erectile dysfn – alprostadil (PGE1)
A.9. Estrogens and antiestrogens - Drugs
ethynylestradiol
estradiol
clomifen
tamoxifen
raloxifen
anastrozole
goserelin
degarelix
A.9 Estrogens and Antiestrogens - Estrogen fn
Estrogen promotes the proliferation of the endometrium and breasts.
Responsible for sexual maturation and growth, secondary charact, female libido.
Endometrial effects – develop of endometrial lining.
Pharma estrogens cause – dec resorption bone, high levels CBG TBG, SHBG, transferrin, fibrinogen, inc HDL, inc TG and cholesterol, enhanced blood coagulation, sodium retention, edema.
SE – postmenu bleeding, nausea, breast tenderness, hyperpigmentation, incre frequency migraine, cholestasis, gallbladder disease, hepatic adenomas.
CI – patients with estrogen based neoplasms, undx genital bleeding, severe liver disease, history thromboembolic disorder, heavy smoker.
ethynylestradiol
synthetic steroidal estrogen.
PO – well absorbed, transdermal, parenteral.
Met CYP450.
TX – parenteral or oral contraceptive, HRT, prevent bone loss and osteoporosis, hypogonadism in girls..
SE – breast cc, endometrial hyperplasia and cc, inc CV risk.
A.9. Estrogens and antiestrogens
estradiol
natural estrogen – main secretory product of the ovary.
Used as IM depot in conjugate form.
First high pass so given transdermal or inject – in the liver forms estrone and estriol.
Binds to SHB and albumin in circulation.
Excretion via bile with enterohepatic recycling
A.9. Estrogens and antiestrogens
clomifen
SERM – selective estrogen receptor modulator.
Ovulation inducing agent. It selectively inhibits estrogen R in the pituitary dec negative feedback causing inc in FSH and LH secretion.
TX – fertility drug.
SE – multiple preg, visual disturb
A.9. Estrogens and antiestrogens
tamoxifen
SERM.
Anti-estrogen.
TX – palliative care of breast cc in postmenu women – hormone responsive breast cc.
SE – hot flashes, thromboembol, inc endometrial cc.
A.9. Estrogens and antiestrogens
raloxifen
SERM.
PO.
TX – tx and prophylaxis osteoporosis in post menu
A.9. Estrogens and antiestrogens
anastrozole
Anti-estrogen.
Non-steroidal inhibitor – Aromatase inhibitor – causes almost total suppression of estrogen synth.
PO.
TX – breast cc resistant to tamoxifen
A.9. Estrogens and antiestrogens
goserelin
GnRH analogue.
Continuous admin of GnRH agonist suppresses GnRH secretion and thereby inhibit ovarian production of estrogens and progestins.
TX – ovulation, suppression women undergoing controlled induction. Ovarian suppression in endometriosis, leiomyoma. Central precocious puberty
A.9. Estrogens and antiestrogens
degarelix
GnRH antagonist.
TX – prevention of premature LH surge in women undergoing controlled ovarian hyperstimulation for assisted reproduction.
SE – prolong QT, heat wave, dec gluc tolerance, dec bone density
A.9. Estrogens and antiestrogens
A.10. Progestins and antiprogestins - Drugs
medroxyprogesteron-acetate
drospirenone
norethisteron
levonorgestrel
desogestrel
cyproteron-acetate
mifepristone
ulipristal acetate
A.10 Progestins and Antiprogestins - function of progestin
natural is progesterone – produced by corpus luteum.
NOT PO, IM admin.
Actions – inhibit proliferation, promote differentiation in:
- endometrium – maturation and secretory changes following ovulation (dec growth inc vascul),
- breast – prolif then alveolobulbar develop of secretory
- implantation, maintenance of preg, inhibition of ovulation
- inc body temp, metabolic
–fat deposition, ketogenesis.
Competes with aldosterone-R so dec Na+ resorption.
Resp – ventilatory response to CO2 inc.
TX – hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress.
SE – inc risk breast cc, dec HDL, impair gluc tole, elevated BP.
medroxyprogesteron-acetate
synthetic progestin, pregnan (21-C cmpd).
Improved bioaval – PO or IM – 150mg every 3 months.
Met CYP450.
TX – primary hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress
A.10. Progestins and antiprogestins
drospirenone
synthetic progestin, pregnan (21-C cmpd).
Improved bioaval – PO or IM – 150mg every 3 months.
Met CYP450.
TX – primary hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress
A.10. Progestins and antiprogestins
norethisteron
is an estran – 19-norsteroid.
Has androgen/anabolic action.
Inhibits implantation – more effective than gonadotropin inhibitors.
PO – minipill.
TX – primary hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress.
A.10. Progestins and antiprogestins
levonorgestrel
gonan. – 13-ethyl derivative of 19-nonsteroid.
High dose can be used as morning after.
Can be used as interuterine device
TX – primary hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress
A.10. Progestins and antiprogestins
desogestrel
gonan. – 13-ethyl derivative of 19-nonsteroid.
PO.
Lower androgen activity than norethisterone.
Used as contraceptive implant with active metabolite etonorgestrel.
TX – primary hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress
A.10. Progestins and antiprogestins
cyproteron-acetate
synthetic progestin, pregnan (21-C cmpd).
Improved bioaval – PO or IM – 150mg every 3 months.
Met CYP450.
TX – primary hypogonadism (HRT), post menu HRT – dec risk endome cc, hormonal contraception, long term ovarian suppress
A.10. Progestins and antiprogestins
mifepristone
19-norsteroid progesterone receptor antagonist.
Terminates early pregnancy when in combo with vaginal PGE1 and its analogue misoprostol – used up to 49 days after last period.
Antiglucocorticoid activity.
Indication – endometriosis, breast cc, meningioma.
SE – vomiting, diarrhea, abdominal pain, vaginal bleeding.
A.10. Progestins and antiprogestins
ulipristal acetate
SPRM – selective progestin receptor modulator.
morning after pill, tx myomas
A.10. Progestins and antiprogestins
A.11. Contraceptives
ethynylestradiol + levonorgestrel
medroxyprogesteron-acetate
levonorgestrel
desogestrel
A.11 Contraceptives - how they work
Oral contraceptives: estrogen+progestin combos.
Effects:
MoA- inhibition of pituitary fn, inhibition of ovulation, changes in cervical mucosa, endometrium, motility, secretion.
Chronic use depresses ovarian fn, and ovary becomes smaller.
Uterus – cervical hypertrophy (polyp formation) thicker cervical mucosa, preps containing 19-norsteroid can cause glandular atrophy, less bleeding.
Breast – enlargement, suppression lactation.
ADVANTAGE – lower incidence of ovarian and endome cc, ovarian cysts, mastopathies. Less bleeding, lower incidence of anemia, improve endometriosis, dysmenorrhea.
DISAD – inc risk vascular disorder – venous thromem, MI, cerebrovascular disor, incr risk GI disorder, depression.
CI – thromboem, cerebrovas, estrogen depen neoplasms, before epiphyseal closure complete. Over 35 and smoke more than 15 cigg. HTN, IHD, breast cc, cirrhosis.
ethynylestradiol + levonorgestrel
monophasic, biphasic 1-10,11-21, triphasic 1-7. 8-14. 15-21.
A.11. Contraceptives
medroxyprogesteron-acetate
parenteral – depot – inject of depot – 150 mg IM – every 3 months.
SE – headache, impair gluc tol, lipid changes, irregular bleeding
A.11. Contraceptives
levonorgestrel
intrauterine device.
DoA 5 yr. daily release, low systemic hormone level.
Can be morning after pill – high dose 0.75 – 1.25mg – within 72 hr sex
A.11. Contraceptives
desogestrel
progestin comonpent.
Its active component etonorgestrel can be used as an implant.
A.11. Contraceptives
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones - Drugs
levothyroxin
thiamazole
propylthiouracil
iodine
octreotide
bromocriptine
desmopressin
oxytocin
levothyroxin
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
thiamazole
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
propylthiouracil
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
iodine
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
octreotide
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
bromocriptine
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
desmopressin
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
oxytocin
A.12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones
A.13. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM.
regular insulin
lispro insulin
glargin insulin
isophan (NPH)-insulin
liraglutide
regular insulin
A.13. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM.
lispro insulin
A.13. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM.
glargin insulin
A.13. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM.
isophan (NPH)-insulin
A.13. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM.
liraglutide
A.13. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM.
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus. - Drugs
glipizide
glimepiride
repaglinide
metformin
vildagliptin
dapagliflozin
acarbose
glipizide
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
glimepiride
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
repaglinide
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
metformin
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
vildagliptin
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
dapagliflozin
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
acarbose
A.14. Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus.
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis. - Drugs
cholecalciferol
teriparatide
raloxifen
zoledronate
alendronate
denosumab
cholecalciferol
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis.
teriparatide
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis.
raloxifen
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis.
zoledronate
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis.
alendronate
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis.
denosumab
A.15. Agents affecting bone mineral homeostasis (calcium, vitamin D, parathyroid hormone, calcitonin, etc.). Pharmacotherapy of osteoporosis.
A.16. Drugs used in coagulation disorders I: Antiplatelet agents
acetylsalicylic acid
clopidogrel
prasugrel
ticagrelor
abciximab
acetylsalicylic acid
A.16. Drugs used in coagulation disorders I: Antiplatelet agents
clopidogrel
A.16. Drugs used in coagulation disorders I: Antiplatelet agents
prasugrel
A.16. Drugs used in coagulation disorders I: Antiplatelet agents
ticagrelor
A.16. Drugs used in coagulation disorders I: Antiplatelet agents
abciximab
A.16. Drugs used in coagulation disorders I: Antiplatelet agents
A.17. Drugs used in coagulation disorders II: Anticoagulant drugs
heparin
dalteparin
bivalirudin
warfarin
dabigatran-etexilate
rivaroxaban
fondaparinux
heparin
A.17. Drugs used in coagulation disorders II: Anticoagulant drugs
dalteparin
A.17. Drugs used in coagulation disorders II: Anticoagulant drugs
bivalirudin
A.17. Drugs used in coagulation disorders II: Anticoagulant drugs