Block 11 Pharmacology Flashcards Preview

Pharmacology > Block 11 Pharmacology > Flashcards

Flashcards in Block 11 Pharmacology Deck (15):
1

Folic acid (Vitamin B9)

DNA precursor

Uses: treatment and prevention of folate deficiencies and megaloblastic anaemia. Prevents neural tube defects in growing foetus

MOA: Converted to tetrahydrofolic acid/ methyltetrahydrofolate by dihydrofolate reductase (DHFR) -> needed for EPO synthesis and purine/pyrimidine synthesis

2

Desogestrel/Etonogestrel / Levonorgestrel

Synthetic progesterone

Uses: Oral contraceptive pill or treatment of endometriosis

MOA: Progesterone Nuclear Receptor Agonist -> slows GnRH release from hypoT reducing the pre-ovulatory LH surge and maintains high levels of progesterone -> SUPPRESSES OVU
LATION

Note: in high doses levonogestrel can be used as emergency contraception

note: Can also be given in a combined pill (progesterone and oestrogen)

3

Oxytocin

Synthetic hormone/ GPC oxytocin receptor agonist

Uses: Induces labour (stimulate contraction of uterine smooth muscle, used in delivery and immediately postpartum)

MOA: Activates uterine receptors to increase intracellular calcium, activate myosin's light chain kinase, and therefore cause muscle contraction.

note: Oxytocin after labour often associated with lactation

4

Ethinylestradiol/Oestradiol

Ostradiol: type of naturally occurring ostrogen hormone

Enthiylestradiol: A synthetic form of oestradiol

Uses: contraceptive pill

MOA: Bind oestrogen receptor causing translocation to nucleus and regulation of gene transcription -> increases synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), suppresses follicle-stimulating hormone (FSH) -> prevents ovulation

5

Dinoprostone

Prostaglandin E2 -> Prostaglandin receptor agonist

Uses: Given as a vaginal suppository to soften the cervix in labour and induce labour,

MOA: stimulates the myometrium of the uterus to contract (exact mechanism unknown)

6

Flucloxacillin

Beta-lactam antibiotic (transpeptidase inhibitor)

Uses: Usually Gram + bacteria but also Gram - bacteria. Also stable against bacteria producing beta lactamase

MOA: Bactericidal. Inhibits bacterial cell wall synthesis by binding to specific penicillin-binding proteins (PBPs) located inside the cell wall. Cell lysis occurs via autolytic enzymes such as autolysins

Note: Commonly used in place of methicillin

7

Tetracycline

A 30s inhibitor (antibiotic)

-A broad-spectrum antibiotic
-Used to treat many infections, including acne.

Uses: infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.

-MOA inhibition of bacterial cell growth by binding to the 30S ribosomal subunit.
-Prevents tRNA from binding ribosome site
- Inhibition of translation

note: Rarely used, replaced by doxycycline

8

Ampicillin

Beta-lactam antibiotic (transpeptidase inhibitor)

Uses: Gram positive bacterial infections

MOA: Inhibits bacterial cell wall synthesis by binding to specific penicillin-binding proteins (PBPs) located inside the cell wall. Cell lysis occurs via autolytic enzymes such as autolysins

note: replaced by amoxicillin now

9

Sodium valproate

Anti-convulsant (GABA receptor agonist)

Uses: Anti-epileptic (control absence seizures, tonic-clonic seizures grand mal and complex partial seizures) and mood stabiliser (in mania)

MOA largely unknown: Increased brain conc of GABA, also block reuptake of GABA. may inhibit enzymes that catabolise GABA

10

Ethanol

A neuronal depressant

Uses: Recreational use, Not really used therapeutically

MOA:
-binds NT receptors for Ach, serotonin, GABA and glutamate
-sedative effect via GABA and glycine receptor binding
- dehydrating agent -> disrupts osmotic balance

11

Cocaine

Noradrenaline reuptake inhibitor/ sodium channel blocker - Local anaesthetic

Uses: Recreational, Local/topical anaesthesia of mucous membranes (oral, laryngeal, nasal), though little clinical use now.

MOA:
-Reversibly binding/inactivating sodium channels, preventing depolarisation of nerve cell membranes and therefore blocking the propagation of impulses along the nerve
-Vasoconstrictive properties via inhibition of NA reuptake
-Addictive properties due to inhibition of dopamine reuptake

12

Lithium

A mood stabilising agent (Sodium analogue)

Uses: Treatment of bipolar disorder (counteracts mania and depression)

MOA unknown: Lithium ion Li+, has a smaller diameter so can easily displace K+, Na+ and even Ca+2 occupying their sites in several critical neuronal enzymes and neurotransmitter receptors

13

Thalidomide

Immunomodulatory agent (immunosuppressive and anti-angiogenic)

Uses: Cancer and leprosy

MOA: suppression of TNF-a reducing inflammation. Also VEGF inhibitor so decreased angiogenesis important to inhibit in cancer

14

Testosterone

Steroid sex hormone (androgen receptor agonist)

Uses: in males with too low testosterone levels, breast cancer
-Function in men: stimulate spermatogenesis, maturation of spermatozoa, support development of secondary sexual characteristics, stimulate overall growth and influence brain development by stimulating sexual behaviours

MOA: Reduced to 5-DHT or activates androgen receptors -> influences gene transcription

15

Somatropin

Synthetic human growth hormone -> hGH receptor agonist

Uses: To treat dwarfism and growth failure

MOA: Binds human growth hormone -> causes dimerisation and activation of JAK2 pathway signalling -> increase in growth and change in metabolism