Flashcards
Pharmacology 3 Test 2 Drug List
Flashcards do conjunto (52)
- 1ClomipheneIndication: Infertility
Competitively antagonises estrogen receptors in the hypothalamus. This interferes with normal negative feedback mechanisms and increases the release of pituitary gonadotrophins, especially LH, inducing ovulation. - 2Gonadotrophinindication: infertility
gonadotrophins stimulate follicular growth; help stimulate ovulation by triggering release of egg from the follicle - 3sildenafilindication: ED
Class: phosphodiesterase 5 inhibitor
(PDE5 inhibitor)
Sexual stimulation increases cyclic guanosine monophosphate (cGMP) levels, resulting in smooth muscle relaxation, inflow of blood to the corpus cavernosum and penile erection.
These agents inhibit the breakdown of cGMP by phosphodiesterase 5 (PDE5), increasing blood flow to the penis during sexual stimulation. - 4tadalafilIndication: ED, also for BPH
Class: Phosophodiesterase 5 Inhibitor (PDE5 inhibitor)
Sexual stimulation increases cyclic guanosine monophosphate (cGMP) levels, resulting in smooth muscle relaxation, inflow of blood to the corpus cavernosum and penile erection.
These agents inhibit the breakdown of cGMP by phosphodiesterase 5 (PDE5), increasing blood flow to the penis during sexual stimulation. - 5testosteroneclass: androgen
Bind to and activate androgen receptors that regulate androgen-responsive genes involved in the development and maintenance of masculine sexual characteristics.
In male hypogonadism, androgen replacement with testosterone is important to prevent long-term complications, such as fragility fractures, and to maintain sexual function - 6ProgestogenProgestogens are Class of drug:
When used as contraceptives, progestogens thicken cervical mucus to impede the passage of sperm and change endometrium, reducing the potential for implantation. They act on the hypothalamus and suppress pituitary LH surge and may inhibit ovulation. Depot injection and implant reliably suppress ovulation; oral progestogen-only contraceptive suppresses ovulation in <50% of women.
Progestogens also induce atrophy within ectopic endometrium. - 7OestrogenHRT
Estrogen relieves symptoms (eg hot flushes, night sweats and urogenital atrophy), caused by reduced endogenous estradiol production. Progestogen reduces risk of endometrial cancer associated with unopposed estrogen. - 8HRT GuidelinesOestrogen ultra-low dose orally, increasing to oestrogen low, medium or high dose
• either orally or transdermally as tolerated or required(‘implant’ preparations also available)Plus the corresponding progestogen dose orally (or transdermally), either cyclical (minimum 10-12 days/ mth or continuous)
Overall, regimens may be oral only OR
combination of oral and transdermal
Low dose COC may be suitable HRT for woman < 50 years who are still requiring contraception
Women without a uterus are safe to just have the oestrogen without progesterone - 9MedroxyprogesteroneProgestogen of choice in HRT
also Progestogen depot as contraceptive
• 99.8% effective
• Intramuscular injection
• Medroxyprogesterone acetate
• Administered every 12 weeks - 10EtonogestrelProgestogen
Used in hormonal contraception, primarily Implanon and Nuva Ring
Less androgenic, does not cause a decrease in sex hormone-binding globulin levels
When used as contraceptives, progestogens thicken cervical mucus to impede the passage of sperm and change endometrium, reducing the potential for implantation. They act on the hypothalamus and suppress pituitary LH surge and may inhibit ovulation. Depot injection and implant reliably suppress ovulation; oral progestogen-only contraceptive suppresses ovulation in <50% of women.
Progestogens also induce atrophy within ectopic endometrium. - 11LevonogestrelProgestogen:
Oral ECP and IUD
Give levonorgestrel as soon as possible after unprotected intercourse, as its efficacy decreases with time. Give it within 96 hours (4 days) afterwards, but preferably within 72 hours (3 days). Levonorgestrel can still be considered 96–120 hours (4–5 days) afterwards (as its risks are minimal) but its efficacy is uncertain.
It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system
also used in COCPs - 12Ethinyloestradioloestrogen
used in CCVR (nuva ring) with Etonogestrel
All COCs contain an estrogen and progestogen. They inhibit ovulation, reduce receptivity of endometrium to implantation and thicken cervical mucus to form a barrier to sperm. - 13Oestradioloestrogen
used with dienogest for COC
All COCs contain an estrogen and progestogen. They inhibit ovulation, reduce receptivity of endometrium to implantation and thicken cervical mucus to form a barrier to sperm. - 14Norethisteroneprogestogen
Norethisterone (NET), also known as norethindrone, is a medication that is used in combination with estrogen or alone in hormonal contraceptives, hormone replacement therapy, and in the treatment of gynecological disorders. It is a synthetic progestogen (or a progestin) , has similar effects to those of natural progesterone, including suppression of gonadotropins, ovulation inhibition, and endometrial transformation. - 15TiboloneHRT
Acts as an estrogen on vagina, bone and thermoregulatory centres in brain. Has progestogenic and anti-estrogenic effects on breast and endometrium. Androgenic effects include decrease in HDL, triglycerides and lipoprotein(a). - 16OctreotideClass: Somatostatin Analogue
Indication: used for the treatment of growth hormone-secreting tumours (in acromegaly) and for other neuroendocrine tumours)
Inhibit release of growth hormone and of various peptides of the gastroenteropancreatic endocrine system (including insulin); have a more prolonged duration of action than somatostatin (natural growth hormone inhibiting peptide). Reduce splanchnic blood flow. - 17Levo-thyroxinelevo-thyroxine (l-isomer of T4) is often the drug of choice for thyroid hormone deficiency
half-life of 6 days, so can be administered once/day - 18liothyroneliothyronine (l-isomer of T3)
shorter half-life (1 day) and faster-acting useful in myxoedema coma/crisis
eg if a patient with long-standing hypothyroidism overwhelmed - 19Carbimazolepro-drug -> methimazole
Indication: hyperthyroidism
Block thyroid hormone synthesis; compete for oxidized iodide in the synthesis process of thyroid hormones - 20PropylthiouracilIndication: hyperthyroidism
Block thyroid hormone synthesis; propylthiouracil also inhibits peripheral conversion of T4 to T3.
compete for oxidized iodide in the synthesis process of thyroid hormones - 21Colecalciferolpurpose is to Regulate calcium homeostasis and bone metabolism. Increase intestinal absorption and renal reabsorption of calcium and phosphate. Promote bone mineralisation.
colecalciferol (vit D3) synthesized in the skin from a cholesterol precursor in response to sunlight (UV irradiation)
colecalciferol is stored and then partly metabolized in the liver
in proximal tubule of kidney, it converts to, Calcitrol, the active hormone - 22Ergocalciferolergocalciferol (vitamin D2) used for vitamin D supplementation
ergocalciferol (vitamin D2) was previously available in OTC vitamin and mineral products but most products now contain colecalciferol. Doses of ergocalciferol and colecalciferol are the same
purpose is to Regulate calcium homeostasis and bone metabolism. Increase intestinal absorption and renal reabsorption of calcium and phosphate. Promote bone mineralisation. - 23calcitoninCalcitonin is a natural hormone involved in calcium regulation and bone metabolism. It inhibits bone resorption and increases urinary excretion of calcium and phosphate.
secreted from the parafollicular cells of the thyroid gland
stimulated by increase in calcium levels above normal physiological levels
binds directly to a G protein-coupled receptor on osteoclasts (and inhibits their activity), also inhibits renal tubular reabsorption/ promotes excretion of both calcium and phosphate in urine - 24Calcium carbonateCalcium carbonate is the most common calcium supplement used
calcium carbonate tablets should be taken with meals to enhance absorption as calcium carbonate requires acidity for optimal dissociation
CaCO3(s) + H+ → Ca2+ + CO2 + H2O
clinical effect may thus be reduced in by drugs which increase gastric pH (eg PPIs, H2 antagonists) by reducing gastric acid secretion - 25Calcitriolbiologically active form of vitamin D
increases calcium absorption from the intestine
main effect on bone is mobilizing Ca2+ to increase Ca2+ levels (promotion of resorption) – this is a physiological process
IN CONDITIONS OF VITAMIN D DEFICIENCY with accompanying impaired mineralization, the main effect of Vitamin D administration is enhanced bone formation
MOA?
unclear, but may be due to stimulus of production of osteocalcin, the protein in the bone matrix which picks up and binds Ca2+. - 26When is calcitriol used directly as a pharmacological entity?In those conditions of Vitamin D deficiency in which (due to some pathology) Vitamin D cannot be converted to the active hormone (calcitriol), That is, if Vitamin D cannot be used to treat Deficiency, then calcitriol is administered directly. Such conditions include:
renal disease (eg patients requiring chronic dialysis)
hypoparathyroidism
Also used in some osteoporotic patients.
* Needs careful monitoring because risk of hypercalcaemia. - 27Alendronateclass: biophosponate
Decrease bone resorption by inhibiting osteoclasts
bind strongly to the mineral content of the bone
as the osteoclasts resorb bone, they are exposed to high concentrations of the drug (i.e. greatest effects on osteoclasts).
due to importance of resorption in bone fracture repair, delayed or absent fracture healing may be an issue in long term users of anti-resorptives
that is, if bone resorption is strongly inhibited, microdamage might not be repaired and damage could accumulate
also, as bone mineralisation increases (due to decreased resorption), bone may become brittle accumulate in bone and remain bound to bone for long periods
duration of effect following cessation of therapy is unclear, but may be in the order of years hence dosed once weekly (but could be, say, yearly)
poor oral bioavailability
even lower if taken with food or liquids other than water, due to affinity with minerals in food and drink
not administered at the same time as calcium supplements - 28Teriparatideprevent bone loss
is a recombinant fragment of human PTH
parathyroid hormone generally promotes bone resorption
However, if given in low /intermittent doses, PTH (or this active fragment – above) paradoxically causes osteoblast –like activity1 2 (thus increasing bone formation) preferentially over bone resorption (anabolic effect)
increases number of osteoblasts, activates those present, decreases osteoblast apoptosis
bisphosphonates may be started after use stopped; use together is not currently recommended – may reduce teriparatide effectiveness - 29strontium ranelateprevent bone loss
stimulates bone formation and decreases bone resorption
combines anti-catabolic and anabolic effects ("dual action
bone agent")
Mechanism not well understood.
Has been hypothesized that it could act as an agonist of the extracellular calcium–sensing receptor important in osteoblast development. - 30orlistatclass: pancreatic lipase inhibitor
Indication: weight loss
Inhibits GI lipases, preventing absorption of approximately 30% of dietary fat.
n addition to helping reduce weight, orlistat has been shown to also:
– Lower plasma low-density lipoprotein cholesterol (LDL) cholesterol levels.
– Cause decline in LDL cholesterol is greater than that expected due to weight loss alone
– Lower HbA1C in diabetic patients
** vitamin ADEK deficiency risk**
fatty diarrhoea - 31LiraglutideClass:glucagon-like peptide‐1 analogue
indication: weight loss
Analogues of glucagon-like peptide‐1 (an incretin); increase glucose-dependent insulin secretion and suppress inappropriate glucagon secretion. They also delay gastric emptying, which slows glucose absorption, and decrease appetite
Adjunct to lifestyle modification in obesity (BMI >30) or in overweight people (BMI >27) with at least 1 weight-related comorbidity - 32Phentermine (duromine is brand name)Weight Loss
Sympathomimetic with CNS stimulatory effects, increasing energy expenditure.
pharmacology similar to amphetamine. It is used medically as an appetite suppressant:
• Stimulate NA release
• Block NA re-uptake
• Increases sympathetic
stimulation
• Also affects DA - 33MirtazapineClass; tetracyclic
Indication: depression
Tetracyclic antidepressant; acts by postsynaptic blockade of serotonin 5HT2 and 5HT3 receptors and presynaptic blockade of central alpha2-adrenergic inhibitory autoreceptors. It is also a potent H1 antagonist which accounts for its sedative effects. - 34AmitriptylineClass: TCA
Indication: Depression
TCAs inhibit reuptake of noradrenaline and serotonin into presynaptic terminals. Although unrelated to the therapeutic effects of the TCAs, they also block cholinergic, histaminergic, alpha1-adrenergic and serotonergic receptors.
withdrawal effect: cholinergic rebound: hypersalivation, runny nose, abdominal cramping, diarrhoea, sleep disturbance - 35Fluoxetine (Prozac)Class: SSRI
Indication: Depression
SSRIs selectively inhibit the presynaptic reuptake of serotonin (5‐hydroxytryptamine, 5HT).
Selectively block serotonin reuptake pump • Immediately increase 5HT in synapse
• Take 4-6 weeks to work
• Most metabolised by CYP450 enzymes
• Fewer SEs than TCAs
• Less sedating
• Less anti-muscarinic effects - 36VenlafaxineClass:SNRI
Indication: Depression
Inhibit serotonin and noradrenaline reuptake.
Inhibition of 5HT, NA & DA reuptake
•At low doses acts like SSRIs
•Intermediate to high doses effects on NA become important
•Cross between SSRI and TCA •Metabolised to desvenlafaxine (active
metabolite, also given as a drug) - 37ReboxetineCLASS:
Indication: depression
Inhibition of 5HT, NA & DA reuptake
•At low doses acts like SSRIs
•Intermediate to high doses effects on NA become important
•Cross between SSRI and TCA •Metabolised to desvenlafaxine (active
metabolite, also given as a drug) - 38PhenelzineClass: NRI
Indication: depression
•Inhibits NA reuptake
•Weakly inhibits 5-HT reuptake •Antagonist at alpha-2 receptors - 39Moclobemideindication: depression
atypical antidepressant
Moclobemide competitively and reversibly inhibits monoamine oxidase (MAO); it is relatively selective for type A (MAO‐A). Synaptic concentrations of serotonin, noradrenaline and dopamine are increased. - 40Clozapineatypical antipsychotic
indication: schizophrenia
Bind better to D2 receptors in parts of the brain that control psychosis than in those that cause the above side effects. Do so by either blocking serotonin or competing loosely with it - 41OlanzapineAntipsychotic actions are thought to be mediated (at least in part) by blockade of dopaminergic transmission in various parts of the brain (in particular the limbic system). Evidence suggests:
all effective antipsychotics block D2 receptors
differential blockade of other dopamine receptors (eg D1) may influence therapeutic and adverse effects
antagonism of other receptors may influence antipsychotic activity, eg 5HT2 antagonism with some agents.
weight gain +++ - 42Chlorpromazinetypical antipsychotic
most sedating; most potent anticholinergic effects; least likely to cause EPSE; most likely to cause orthostatic hypotension; sometimes referred to as ‘low potency’ antipsychotics
Antipsychotic actions are thought to be mediated (at least in part) by blockade of dopaminergic transmission in various parts of the brain (in particular the limbic system). Evidence suggests:
all effective antipsychotics block D2 receptors
differential blockade of other dopamine receptors (eg D1) may influence therapeutic and adverse effects
antagonism of other receptors may influence antipsychotic activity, eg 5HT2 antagonism with some agents. - 43Haloperidoltypical antipsychotic
least sedating; almost no anticholinergic effects; most likely to cause EPSE; least likely to cause orthostatic hypotension; sometimes referred to as ‘high potency’ antipsychotic
Antipsychotic actions are thought to be mediated (at least in part) by blockade of dopaminergic transmission in various parts of the brain (in particular the limbic system). Evidence suggests:
all effective antipsychotics block D2 receptors
differential blockade of other dopamine receptors (eg D1) may influence therapeutic and adverse effects
antagonism of other receptors may influence antipsychotic activity, eg 5HT2 antagonism with some agents. - 44lithiumits actions include inhibition of dopamine release, enhancement of serotonin release and decreased formation of intracellular second messengers. Lithium has little or no psychotropic effect in normal individuals.
Mood stabilizers are medications that help control the highs and lows of bipolar disorder. They are the cornerstone of treatment, both for mania and depression. Lithium is the oldest and most well- known mood stabilizer. Lithium takes from one to two weeks to reach its full effect.
Lithium closely resembles sodium and substitute for sodium as a charge through sodium channels. However, lithium is not pumped out as quick as sodium by the Na+/K+ – ATPase. This results in an intracellular accumulation of lithium, a partial loss of intracellular potassium and a partial depolarization of cells.
Consequently, lithium inhibits depolarization-evoked neurotransmitter release (noradrenaline & dopamine).
In addition, lithium inhibits several enzymes involved in the normal recycling of membrane phosphoinositol. This results in a depletion of PIP2, the precursor for IP3 and DAG - 45valproMultiple mechanisms. Prevents repetitive neuronal discharge by blocking voltage‐ and use-dependent sodium channels. Other actions include enhancement of GABA, inhibition of glutamate and blockade of T-type calcium channels.
in bipolar:
Valproate and carbamazepine are used as alternatives when lithium is considered poorly tolerated or ineffective; they are sometimes used with each other or with lithium. Valproate and carbamazepine also appear to be particularly suitable for those with rapid cycling illness (4 or more episodes a year) - 46lamotrigineStabilises presynaptic neuronal membranes by blocking voltage-dependent and use-dependent sodium channels and inhibiting glutamate release.
Prevention of depressive episodes - 47carbamazepinePrevents repetitive neuronal discharges by blocking voltage-dependent and use-dependent sodium channels.
Valproate and carbamazepine are used as alternatives when lithium is considered poorly tolerated or ineffective; they are sometimes used with each other or with lithium. Valproate and carbamazepine also appear to be particularly suitable for those with rapid cycling illness (4 or more episodes a year). - 48olanzapine for bipolaruse in combo with mood stabiliser
- 49sumatriptanClass: triptan
Indication: migraine
Constrict cranial vessels by acting selectively at 5HT1B/1D receptors; also thought to inhibit the abnormal activation of trigeminal nociceptors.
for migraine
Relieves pain of migraine and associated symptoms • 3 dosage forms: oral, nasal, & parenteral
• Low oral bioavailability (14%)
• Half life of 2.5 hours
hydrophilic triptan, based on several animal studies has been regarded to be unable to cross the BBB. In more recent animal studies there are strong indications that sumatriptan to some extent can cross the BBB. That applies to all of the migraine drugs. - 50ZolmitriptanClass: triptan
Indication: migraine
Constrict cranial vessels by acting selectively at 5HT1B/1D receptors; also thought to inhibit the abnormal activation of trigeminal nociceptors.
Oral bioavailability improved to ~50%
• Half-life of 3 hours
• Taken orally at the onset of headache pain - 51NaratriptanClass: triptan
Indication: migraine
Constrict cranial vessels by acting selectively at 5HT1B/1D receptors; also thought to inhibit the abnormal activation of trigeminal nociceptors.
Oral bioavailability improved to ~60%
• Half-life of 5-6 hours
• Take orally at the onset of headache pain - 52ErgotamineStructurally similar to amines, serotonin, norepinephrine, and dopamine
• Interact with multiple receptors in these systems (less specificity)
• Cause constriction of the blood vessels
• Wide-range of effects
• Partial agonist of alpha adrenergic and 5-HT1 and 5HT2 receptors
• Problems: avoid if patient has coronary disease; safety margin is small; overdose dangerous
• Probably crosses BBB
• 1% bioavailability
The mechanism of action of ergotamine is complex. The molecule shares structural similarity with neurotransmitters such as serotonin, dopamine, and epinephrine and can thus bind to several receptors acting as an agonist. The anti-migraine effect is due to constriction of the intracranial extracerebral blood vessels through the 5-HT1B receptor, and by inhibiting trigeminal neurotransmission by 5-HT1D receptors. Ergotamine also has effects on the dopamine and norepinephrine receptors. Its side effects are due mainly to its action at the D2 dopamine and 5-HT1A receptors
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- pharmacology (pharmacology 3) FlashCards sobre Pharmacology 3 Test 2 Drug List, criado por Amelia Claire em 11-10-2017.
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- Amelia Claire
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