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118 Cards in this Set
- Front
- Back
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What are common conditions caused by histamine in the body?
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hayfever, rhinitis, itcihng, hives.
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What can anithistamines be used for?
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Decreasing allergic response
Antiulcer drugs Motion sickness Mild sedatives |
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What are three types of eicosanoids?
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Prostaglandins, Luekotrienes and Thromboxanes
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What effects on the body do eicosanoids have?
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Inflammation and pain
Senstise nerve endings to pain Capillary permeability Chemotaxis Induce vasodiln/heat |
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What are some conditions Leukotrienes cause?
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Asthma
Rheumatiod arthritis Psoriasis Ulcerative colitis |
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What do thromboxanes do?
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Involved in platelet agrgn
Produce thrombus Effect vascular diameter |
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How do anti inflam durgs work?
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By blocking phospholipase
by blocking cyclooxygenase (lukotriene recep antags in asthma) they: < fever, pain, inflam, clotting |
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What are some common NSAIDs?
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Aspirin
Paracetamol Ibuprofen Piroxicam Indomethacin |
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How does aspirin work?
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Aspirin blocks COX enzymes
(cox 1 = cell signal&platelet aggrn) (cox2 = inflam pathway) salicylates acetylate cox enzs |
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What are aspirins two main roles?
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non steroidal anti inflam
inhibitor of platelet aggrgn (does not break down clots!!) |
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What do corticosteriods do?
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They are immune suppresant and anit inflammatory drugs
Work by inhibiting phospholipase 2 EG Prednisolone |
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Drugs that stimulate immunity
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Antiserum, provides anitbodies for patients with no pre existing immunity. EG diptheria, rabies.(allergic rxns occur)
Vaccines, sensitize immune cells EG tetanus,hepatitis |
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What are some drugs that are used to supress immunity?
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corticosteroids
cyclosporine tacrolimus |
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How does aspirin inhibt clot formation?
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in platelets, only cox 1 is detectable. so aspirin blocks cox 1 within 1 hr of oral admin, stopping thromboxane a2 for entire palelet life.
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Cox 2 only inhibitors?
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stop pain, fever inflam, whithout GI/ renal injury
EG celebrex |
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what types of drugs are used to treat haemostasis?
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Antiplatelets: NSAIDs, Diprymadole
Thrombolytic: streptokinase Anticoagulant: Heparin, Warfarin |
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what are the side effects of NSAIDs?
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GIT disturbances
Skin rxns Adverse renal effects Respiratory disorder Metabolic acidosis |
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What are the symptoms of aspirin disorders?
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Ringing in ears
Rapid breathing, vomiting,dehydration, fever dizziness |
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What are the newer types of antiplatelet drugs?
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ADP receptor antag=prevents fibrinogen binding
GP11b/111a recep antag=blocks binding fibrinogen and clotting factors |
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Pharmacological treatment for stroke?
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Anticoagulatnts=warfarin
Antiplatelet=aspirin Thrombolytics=streptokinase |
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CNS PHARMACOLOGY
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drugs modulating behaviour, cognition, motor activity. anxiolyics, antipsychotics, sedatives, antidepressants, antiseizure drugs.
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Blood brain barrier
(ths CNS drugs normally able to cross BBB) |
bain capillaries tightly connected to each other, surr by astrocytes. selectively permeable to water, gases, ethanol and lipid sol molecules.
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CNS neurotransmitters
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Monoamines:Noradrenaline, Adrenaline, Dopamine, Serotonin, Histamine.
Inhibitory: GABA Excitatory: Glutamate also: Ach. |
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Dopamine
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behaviour, hormonal release, motor control, vomiting, addiction, mood, nerves.
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Acetylcholine
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cognition and memory, motor function, implicated in Alzheimers and Parkinsons.
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Noradrenaline
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Arousal, sleep, mood, appetite, temperature control, hormone release.
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Seratonin
GABA |
Behaviour, mood, eating
Inhibitory, < acitvity. |
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how can CNS drugs effect NTs?
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Synthesis
Storage Release Breakdown Reuptake in nerve terminal |
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Types of mental disorders
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Schizophrenic
Anxiety Mood disorders Organic mental disorders Sleep disorders Others: eating disorders etc |
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hypnotics and sedatives
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used for insomnia, anxiety and as general anaesthetics.
EG Benzodiazepines, Barbiturates |
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Barbiturates-how do they work
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Hypnotic & Sedative
Acts on GABA, fast inhibitory action, < motor activity & anxiety CNS depressant (ie <respirn) |
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Barbiturates-what are the effects of?
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Loss of conciousness without pain relief!
low therap index = dangerous death due to resp and CV deprn Pharmacokinetic tolerance devel |
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Benzodiazepines-how do they work?
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Facilitates binding of GABA
action = hypnotic, anxiolytic, anticonvulsant, sedatvie, musc relaxant. EG midazolam, diazepam |
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Benzodiazepines -what are the effects of
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< anxiety, <aggression
sedation relaxation Anticonvulsant |
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Adverse rxns of Barbits and Benzos
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CNS depression
resp depression drowsy, mem loss, confusion Dont mix with alcohol or other cns depressants Tolerance and dependance can occur! |
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Schizophrenic/ psychosis disordes. what diseases can present like these disorders?
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metabolic and endocrine disorders, brain tumor, cerebrovasc diseas, hypoglyc, MS, <vit b12
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What drugs can mainfest symptoms?
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Ampehtamines
Benzos Beta blockers Levodopa Steriods Anitcholinergics |
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What are Neuroleptic(antipsychotic) drugs used for?
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they are major tranquillisers that antagonize dopamine receptors
used for symptoms of psychoses, schizophrenia. just relieve sypmtoms. |
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what are the three main groups of chemicals used as Neuroleptics?
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Phenothiazine = Largactil
Thioxanthene =chlorprothixine Butyrophenone = Haldol/ Serenance |
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Typical Antipsychotics (work on dopamine receps)
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Largactil
Haldol Modecate Aldazine |
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Atypical Antipsychotics (work by different mechs)
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Clozaril
Zyprexa Risperdal can help to < side effects or work in ppl resistant to Antisyc |
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Side effects of Antipsychotics?
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these drugs also block other NTs
Apathy, < initiative poor compliance involuntary movt(ie shakes) endocrine effects dry mouth, urine retention liver, skin + eye changes |
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Mood stabilisers
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Lithium salts
Mehcanism of action unclear, controls mania, prevents mood swings, low therap index, adverse rxns |
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Stimulants
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> effects of catecholamines(Ad/NAd)
Amphetaimes & Methylxanthins |
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Antidepressants, what are the four types?
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Tricyclic Antidepressants
Serotonin/ NAd selective reuptake inhibs Monoamine oxidase inhibs Atypical antidepressants |
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Tricyclic antidepressants
how do they work, side effects |
block reuptake of NAd into nerve terminal.
SE= sedation, confusion may block other recps, dont mix with alcohol/ antihypertensives |
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Selective re uptake inhibs
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Serotonin sel reups: prozac, aropax, zoloft
Serotonin/NAd sel reups: efexor SE= nausea, insomnia |
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MOAI's: two types A and B
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A:in liver, gut+brain
B:most in brain Site of action:NAd/ Serotnin synapses |
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what foods cant patients on MAOIs eat?
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Tyramine rich foods such as cheese, wine, beer, chocolate, bananas.
Causes hypertension! |
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what are the side effects of antidepressants?
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tricylclic:antimusc, antiadrenergic effects
Selec sero/NAd reuptakers: headache nausea vomiting insomnia MAOI:Nausea, dietry restriction(hypertensive crisis) insomnia |
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Epilepsy describe?
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electrical discharge across cerebral cortex(nerves firing)
focal, diffuse, partial, generalised seizure tonic/clonic violent muscle spasm |
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what are the actions of an antiepileptic?
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> GABA action
inhibit Na channel fn inhibit Ca channel fn inhibit Glutamate release all to stop neruon excitability. |
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Types of drugs?
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Hydantoins:< nerve firing
Succinimides:inhib Ca channels Benzodiaz:>GABA Valproic:>GABA Lamotrigine:<glutamate |
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What other drugs can be used for epilepsy?
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Muscle relaxants ie Quinine
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CARDIOVASCULAR SYSTEM PAHRM
What are the major drug groups used? |
B recep blockers
alpha recep blockers Ca channel recep blockers Diuretics ACE inhibs Ang II blockers Cardiac gylcosides |
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Antihypertensives:what do sympatholytics do?
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Block the effects of the symp NS.
<BP by stopping vasoconstrn and >HR caused by SNS. |
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Antihypertensives: what are other drugs?
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Ca channel blockers:inhibit vasoconstrn(works on heart and vasc sm musc)
Nitrates: relax Vasc sm musc |
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Antihypertensives:ACE ihibitors
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blocks ACE acting to make Ang II, prevents vasoconstrn
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Antihypertensives: Diuretics
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Act on kidney tubule to decrease water reabsorption.
different types: loop diures, thiazide diures, K sparring diures(weak) |
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What can pharmacological intervention help with?
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> force of heart contrn
>exrcn salt and h20 relax vasc sm musc inhibit renin angiot system |
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How do cardiac gylcosides work?
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by inhibiting Na/K channels.
> force and efficiency of heart >CO (slows hr giving >time for filling) (only used for CCF) |
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What are the classes of antiarrythmic drugs?
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Class 1: Na channel blockers
Class 2: B-adrenorecep antags Class 3:>durn of Action Pot Class 4: Ca channel blockers |
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What can cause Angina?
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Partial blockage of coronary arteries
Reduced bld flow thru cornary arteries as result of vasospasm |
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What factors effect Myocardial oxygen demand?
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Heart rate
Ventricular wall stress Contractility |
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How do nitrates work?
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Organic nitrates lead to NO prodn. which acts as:
potent vasoconstrictor, inhibit platelet aggrn, stops hardening of arteries. |
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What are the actions of nitrates?
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direct vasodilators
< total periph resistance < systemic Bp used for hypert, angina, cardiac failure |
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Mechanism of action on nitrates?
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taken up by endothelial cells of vessels, converted to NO, NO causes the relaxation of muscle = vasodlin
= < bp, < myoc o2 demand, < in preload and afterload. |
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Use of GTN in pulmonary hypertension?
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Acts on ventilated alveoli, helps to dilate bld vessles in alveoli to reduce respiratory distress.
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Routes of Admin of nitrates?
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Gas
Oral Patches(prophylaxis against angina) Injection (AMI/ LVF) |
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What drugs can be used in MI?
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Thrombolytics, antiplatelets
EG: streptokinase and aspirin others:o2, ca antags, ACE inhibs, B recep antags |
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Heparin, when can it be used?
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fast action, inhibits coagulation.
During pregnancy PE DVT after surgery to prevent clot |
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What are low weight heparins?
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Small isolated from heparin. used at lower doeses, safer, longer acting.
EG enoxaparine |
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What does Wafarin do?
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Prevents formation of venous thrombosis, and pulmonary thromboembolism.
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What are fibrinolytics?
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Used to dissolve blood clots.
catylase action of plasmin. EG streptokinase |
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Hyperlipeademia, what drugs are used to treat this?
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HMG Co A reductase inhibs(Statins:<choles synth)
Bile acid binding resins Nicotinic acid derivs Fibrates derivs combination therapy |
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What kind of endocrine disorders are there?
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hyperthyroidism
hypothyroidism hypoglycaemia ketoacidosis(alcoholic/ diabetic) |
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How do endocrine drugs help?
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Repair a deficincy of specific hormone
Compensate for excess or inapprop effect of spec hormone stimulat/block endocr response |
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What are the throid hormones, what effect do they have?
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TRH-hypothal;
TSH-anterior pit; Release hormones T3 and T4 affect metabolism, cardiac fn, growth, devel, energy. |
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Hyperthyroidism: describe
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Most common cause= Graves disease = > T4 and TSH levels
due to overactive thyroid from >TSH levels. S/S: >nervousnes, >irritated, >HR, >temp, weight loss, fatigue |
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Treatment of hyperthyroid states
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Reduce levels of circulating hormone Via:
Blocking synth Stopping iodine availability EG Propythiouracil, surgical removal |
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Hypothyroidism:describe
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Most common cause is body attacks thyroid gland
S/S Fatigue, weight gain, <temp, dry skin, constipation Diag by >TSH levels Treat by oral T4 |
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Insulin dept Diabetes IDDM
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Juvenile, early onset.
Autoimmune destruction of B cells: ie no insulin made Possibly caused by viral infn followed by immune response agains pancreas. |
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Non-insulin dept Diabetes NIDDM
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Primarily a disease of insulin resistance. ie insulin cannot get into cells.
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Treatment NIDDM
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Diet and excercise
Oral antidiabetes agents: Sulphonyureas: Stim B cell in pancreas to > insulin secrn Biguanides:Impair glu absorp from gut Alpha Glucosidase inhibs:delay glu absorp in gut |
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Diabetic ketoacidosis
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Occurs in Type 1 (IDDM) no insulin leads to hyperglyceamia in bld, cells cant get any so end up acidiotic from fat and protein catabolism.
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Signs of Hyperglycemia
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Thirst, Polyuria, dry skin, dry mucous membrane
Tachycardic,hypot,tachypnea ketone breath, confusion, coma Treat: fluid, insulin admin |
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Alcoholic ketoacidosis: chronic abuse alcohol, low food intake, vomiting
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Gylcogen depleted, so ketones produced as substitute. dehydration increases concentrn of counter reg hormones.
S/S nausea vomiting dizzy, fever,pain, dyspnea |
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What drugs can be included when talking about antimicrobials?
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Antibacterials, Antifungals, Antivirals, Antihelmithics, Antiprotozoals
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How do antimicrobials work?
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-inhibiting cell wall synthesis
-inhibit protein synthesis -inhibit topoisomerase -interference with metabolic processes |
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What is the difference between bacteriostatic and bacteriocidal?
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Bacteriostatic stop the synthesis of DNA, halting the reproduction. Bacteriocidal kill the bacteria by disrupting cell wall and membranes
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What are three adverse reactions to antibacterials?
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Superinfections(if all good bact killed from antibiotics, bad ones multiply++)
Hypersensitivity(Allergic rxns) Resistance(microbes adapt to drugs) |
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How can bacteria decrease the action of antimicrobials?
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-Glycocalyx
-Enzymes:B-lactamase,breaks down part of anitbiotic -Target site altered:drug cant bind, -Efflux pump:intercell drug conc too low -bypass pathways |
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How can the drugs be specific to bacteria and not harm human cells?
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:non toxic to mammalian cells
:specific for structures only in bacteria :differences in biochemical pathways :cell walls in bact |
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Inhibition of cell wall synthesis
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Penicillin
-braod spectrum, semisynthetic,Gram+, some Gram- B-lactam ring combines with enzy normally helping to biuld cell wall. ie stops synth cell wall. |
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Inhibition of cell wall synthesis 2
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Cephalosporins
-braod spectrum Gram+ and Gram- Chem modification on B-lactam ring:gives vast array of cephs(1st, 2nd, 3rd generation)same action as pen |
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Inhibition of cell wall synthesis 3
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Vancomycin-large molecules
Only Gram+(cant get thru -wall) Bind to growing peptide chains of cell wall, stopping synthesis. |
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Inhibition of protein synthesis
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Isolated from Streptomyces mould
Affect ribosomal subunits or nucleus: hence protein synthesis is affected. 3 types |
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Inhibition of protein synth 1
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Macrolides
Bind to 50s ribosomal subunits:prevent rel of tRNA eg erythromycin Gram - & + low toxicity, used in patients allergic to penicillin |
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Inhibition of protein synth 2
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Aminoglycosides
Interfere with 30s sunbunits:misreading of mRNA useful in treatment of sepsis. ie Gram-, Streptomycin adverse rxns:ototoxic, nephrotoxic |
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Inhibition of protein synth 3
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Tetracyclines
prevent attachment of aa to ribosome broad spec: Gram- and + |
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What are the criteria ideal for disinfectants and antiseptics?
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-destructive to microbes, but non toxic to humans
-low incidence of hypersent rxns -be active in presence of soaps -be stable, non-corrosive, non-staining and inexpensive |
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Antiseptics: Oxidising
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-Hydrogen peroxide 3%
fast acting, short lived used for traumatic wounds, also for contact lens cleaning |
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Antiseptics: Oxidising
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-Halogens
antibact actions of gases when in contact with water EG Chlorine: sodium hypochlorite uesd to sterilise equpimt or wound irrigation |
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Antiseptics: Oxidising
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Iodine
kills bacteria, fungus and protozoa used for minor wounds, on skin, for viral infections |
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Heavy metals
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-Silver nitrate 1 %
bacteriocidal in contact with skin. Used for eye, nose throat infn -Mercury -Zinc sulphate:nappy rash |
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Alkylating agents
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Aldehydes
-Formaldehyde-1-10%kills micorbes and spores in 1-6 hrs also for disinfection of equpimt preservation of biological material |
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Affecting cell permeability
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Biguanides
Chlorhexidine (Hibiclens) Both Gram - & + disrupts cell membrane used in surgey scrubs,hand washes, skin clenser, oral rinses |
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Phenols
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Poison if ingested or applied to open wounds
no skin contact if >2% |
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Acohols
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Ethanol:denatures proteins
70%: antiseptic used for disinfn of instruments preparation of skin |
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Antifungals (Antimycotics)
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Inhibit sterol synthesis in fungal cell membr
interfers with permability and transport fns |
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3 Types of antifungals
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Griseofulvin
Imidazole Nystatin |
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Antivirals
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difficult to treat
-inhibit uncoating -interfere with rna/dna synth -interfere with polymerase -ihibit reverse transcriptase |
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3 types of Antivirals
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Acyclovir- herpes simplex
AZT Zidovudine- HIV Amantadine-influenza |
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3 types of Antiihelminthics
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Mebendazole (Vermox)
Thiabendazol Pyrantal (Combantrin) |
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Chemotherapy
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3 major classes
Cell cycle non-specific Cycle specific Tissue specific |
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Name 5 drug types
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Antimetabolites
Alkylating agents Antitumor antibiotics Hormones Mitotic inhibitors |
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What do plant alkaloids do?
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periwinkle plant: act during mitosis
mandrake:increase degredation of DNA |
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what are some side effects of chemotherapy?
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alopecia
irritation immunosuppression anaemias, neuropathies, sterility |
