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pharmacology
| Question | Answer |
|---|---|
| Mixtures | preperations in which drugs are dissolved in water ,Aqoueous,liquid preapration ,orally |
| Decoction | solutions obtained by boiling plants in water |
| Aquae | solutions of volatile oils in distilled water |
| syrup | solutions of sugar containing flavour and colouring , orally aqueos liqid prepeartion |
| Elixirs | ALcholic solution of sugar containg flavour,alcholic liquid orally |
| Spirit | Alcholic solution of volatile drugs ,liquid , orally |
| fluid extract | Hydroalcholic extract of plants (1 ml contain activity present in 1 gm of the crude drug ),alcholic, liquid, orally |
| Tablet | coated by chocolate or sugar ,solid ,orally |
| Enteric coated tablets | A type of tablets ,coated with substances which resist dissolution in stomach and dissolve in intestine to be absorbed |
| Tablets with sustained action | Tablets with slow realease of active drug |
| sublingual tablets | small tablets or pellets placed beneath the tongue which is absorbed by mucosa to systemic circulation |
| capsules | these are shells of gelatin containing individual doses of drugs |
| Hard capsules | contain powdered drugs |
| soft capsule | contain liquid or semiliquid drugs |
| Enteric coated capsule | covered with substances which resist dissolution in stomach and disslove in intestine |
| powders | Type of solid prepearations,orally which contain effervescent granules put in small paper (mixed with sodium bicarbonate , citric acid , and H20 to release CO2) |
| Ampoule | parenterally form (one dose ) |
| Vials | Rubber capped bottles containg (multiple doses) |
| Aerosoles | suspention of fine solid or liquid particles in gas by special inhaling device(spinhaler) |
| ointment | semisolid , fatty or oily absorbed by rubbing |
| Lotions | aqoueous suspention absorbed without rubbing |
| lozenge | tablets for slow dissolution in mouth |
| opthalamic solution | eye drops (sterile , isotonic with tear fluids and non irritant ) |
| cosmetic creams | contain water which evaporates when applied to skin producing cold sensation |
| Rose water | Aquae , aqueous prepartion orally |
| Ammonia | spirit , alcholic preparation orally |
| glycerine | suppository given rectally |
| pessaries or ovules | suppository given into vagina |
| Bougies | suppository given into urethera |
| cyclopropane | gas given through respiratory tracts (general anaesthetic) |
| Amyl nitrite | vapour produce coronary VD |
| Disodium cromoglycate | particles in capsule used in aerosoles by spinhaler device for acute bronchial asthma |
| calamine | a type of lotion |
| Talcum | types of powder used for skin |
| Nitroglycerine | transdermal patch and sublingual drug used for cardiac asthema |
| 1 drop | 1/20 ml |
| 1 dessert spoon | 10 ml |
| 1 tea spoon | 5ml |
| 1 glass | 240 ml |
| Dexamethasone | used for acute urticaria (Ampoule) 8mg/2ml every 12 hr |
| clemastine | tablet used for acute urticaria twice a day |
| calcium gluconate | Ampoule used for acute urticaria 10 ml 10% taken slowely |
| ferrous fumarate | tablet used for anemia 200mg tid after meals |
| septazol suspension | solution used for tonsillitis 2 teaspoons every 21 hr |
| paractemol infant | suppository used for high temp twice a day |
| infiltration anesthesia | infilitration around sensory nerves as trigeminal neuralagia |
| trigeminal neuralgia | التهاب العصب الثالث |
| Antacids | not absorbed by git but has local effect on gut |
| Gut | القناة الهضمية |
| Disadvantages of oral enteral | not suitable for ( emeergency-comatosed-iritant drugs -drugs destroyed-drugs completely metabolized-GIT stability ) |
| morphine | completely metabolized by 1st pass metabolism |
| constipation | امساك |
| propranolol,nitroglycerin | 1st pass metabolism by liver |
| Alpha methyl dopa | 1st pass metabolism by intestinal wall |
| nicotine,isoprenaline | 1st pass metabolism by lung |
| isoprenaline | sublingual drug |
| vomiting | التقيؤ |
| rectal advantages | suitable for(comatosed-child-vomiting -passing without destruction) |
| rectal disadvantages | irritant drugs causes anal polyps |
| anal polyps | اورام حميدة شرجية |
| I.D | used for senstivity test and infilitration anesthesia |
| S.Q | drugs shouldent be irritant to avoid abscess and pain |
| abscess | الخراج |
| insulin | used S. Q |
| implantion of pellet | slow release of hormones |
| I.M | should be mild irritation (muscles are less senstive to pain ) sould be aqueos , suspension , oily |
| IV | should be sterile and free of pyrogen (endotoxin)and aqueos solution and it can be very irritant drug |
| disadvantages of I.V | anaphylactic shock pyrogenic reaction to products of killied bacteria phlebitis transmission of disease -fast reaction (cardiac arrest) |
| aminophylline I.V | rapid injection cause cardiac arrest |
| anaphylactic shock | صدمة الحساسية |
| pyrogenic reaction | fever caused by reaction of endotoxins with bacterial products |
| phlebitis | التهاب وريدي |
| Adrenaline | An antognist, I.C injection directly to the heart as in cardiac arrest |
| I.A | in the lumen of the artery as close as possible to the site of action used in dignosis (arteriogrphy )or therapetic(coronary thrombus ) |
| thromus | جلطة |
| intra articular injection | drug injected in the joint cavity |
| Hydrocortisone | intra articular injection for chronic arthritis |
| chronic arthritis | التهاب المفاصل المزمن |
| intrathecal injection | injectedd in the subarachnoid space to reach CSF as spinal anaesthesia |
| inhaltion | general anesthesia in large surface area (alveolar epithelium) but can cause irritation to pulmonary epithilium |
| scopolamine | transdermal patch |
| Affinity | it is the ability of a drug to bind a receptor |
| Efficacy | ability of a drug receptor complex to produce an effect maximal effect produced if a maximal dose is given |
| Potency | it refers to the concentration or dose of a drug producing specific effect, the smaller EC50 , the greater the potency |
| Agonist | a drug has affinity , high efficacy , and rapid rate of dissociation with its receptor |
| partial antagonist | a drug has affinity, weak efficacy , moderate association and dissociation its effect <full agonist effect,it act as antagonist in the prescence of full agonist |
| Nalorphine | a partial antagonist |
| inverse agonist | an agonist produces the reverse of the normal response |
| beta-carboline | Inverse agonist |
| Antagonist | ligand having affinity , no efficacy and slowly associated and dissociated from the receptor |
| Atropine | An antagonist |
| Graded dose response cure | show the relation between Dose and its response |
| Graded dose curve used to measure | E-max,ED50,potency |
| linear scale of dose curve | Hyperbolic , dose represented on the x-axis |
| semilog scale | sigmoid curve(s-shaped),log dose pf the drug on x-axis |
| E-max | the maximal effect at high drug concentration when all receptors are occupied by the drug (highest limit on y axis ) |
| EC50 | the drug concentration or dose to give the half maximal effect on x-axis |
| Types of sympathetic receptors | a1,a2,b1,b2.b3 |
| beta 1 actions | heart:increase all cardiac properties and C.O.Pand O2 cons. SMF:eye:ciliary epithillium increases aqueos secretion (IOP) other actions:kidney:renin/CNS:sympathetic outflow |
| cardiac properties | (contractility-conductivity-excitiability-heart rate ) |
| beta 2 | CVS:vd of skeletal and coronary blood vessels SMF:eye:increases IOP/bronchi:relaxation /GIT and unirary wall:relaxation /uterus:relaxation other actions :liver-glycogenlysis/skeletal muscles :muscles tremors and increase uptake of K-Hypokalemia |
| IOP | intraoclear pressure |
| CVS | cardiovascular system |
| beta 3 | fat cells : Lipolysis |
| alpha 1 | CVS: V.C of skin and membrane blood vessels SMF:eye:iris ms -mydrasis(dilator pupilae)/GIT and UB sphincter contraction and increse tone male sex organ :ejaculation |
| alpha 2 | inhibitory action :central : dec. sympathetic blood flow presynaptic - decreases NA release |
| MECHANISMS of action of adrenergic receptors | they are G protein coupled receptors |
| Alpha 1 mechanism | Gq proteins :stimulate phosopholipase C-inc . IP3 and DAG from triasylglycelor -increas Ca |
| alpha 2 | Gi proteins : decrease adenyl cyclase -decrease CAMP |
| beta receptors | Gs proteins : stimulate adenyl cyclase - inc ATP -increases CAMP |
| sympathomimetics | Drugs produce actions similar to sympathetic nerve stimulation Structure:(catecholamines-non catecholamine) Action :(Direct-indirect-dual) |
| catecholamines | contains catechol nucleus -not absorbed orally - rapid onset -short duration - can not pass BBB - metabolized by MAO and COMT |
| Adernaline , NOR adernaline .Dopamine, Isoprenaline,Dobutamine | they are catecholamines and direct in action |
| NON catecholamines | DOnt contain catechol nucleus -well absorbed orally-slow onset,long duration,can pass to BBB,not metabolized by MAO or COMT |
| Ephedrine classification | non catecholamines and dual in action |
| Amphetamine , tyramine , cocaine | non catecholamines and indirect in action |
| adrenaline site of action | all receptors |
| adrenaline routs of administration | locally on eye , inhalation , IC, SQ not orally |
| Direct mechanism | effect increased after sympathectomy(supersensitivity) No tachyphylaxis |
| tachyphylaxis | تسارع المقاومة للدواء |
| indirect mechanism | release nor adrenaline from vesicles |
| adrenaline action on CVS | heart:increase cardiac properties and C.O.P and cardiac work Blood vessels:VC of skin and mucos membrane (a1) VD of coronary and skeletal blood vessels (b2) BLood pressure: increase systolic BP with slight variation in diastolic BP |
| systolic | top number |
| disystolic | bottom number |
| adernaline on systemic system | eye:midrasis,(a1)and decongestion, decrease IOP(useful for glaucoma)/respiratory:bronchodiltation B2 and decongestion due to a1 stimulation of mucos membrane blood vessels GIT and UB:relax of wall (b2)-contraction of sphincter (a1) |
| other actions of adrenaline on systemic | sex :ejaculation (a1)-pregnant uterus relaxation (b2) kidney:Renin secretion(b1) /liver:Glycogenlysis(B2) /skeletal ms:inc uptake of K and muscles tremor (b2) and facilitate NM transmission (a1)/fat cells :lipolysis(b3)/CNS:affect sympathetic flow |
| Antiallergic action of adrenalline | adrenaline is physiological antagonist of histamines |
| local effects of adrenaline | VC of cutenous bv (a1): prolong action of local anesthetics VC of conjunctival blood vessles (a1) VC of mucos membrane bv of the nose(a1) :nasal pack for hemostasis in epistaxis/VC of mucos membrane bv of bronchi (a1)andbrochdilator(b2):inhalation |
| therapeutic effects (local uses )of adrenaline | prolong effect of anasethetics by decreasing its absorbtion local hemostasis in epistaxix and bleeding sufaces decongestion of mm of nose and eye :in open angle glaucoma acute bronchial asthma :inhalation |
| therapetic effects (systemic uses )of adrenaline | cardiac resuscitation : intracardiac acute attack of bronchial asthma :SC contraction ring to relax the uterus allergic reactions :anaphylactic shock hypoglycemic coma |
| side effects of adernaline | Tachycardia,palpitation,arrhythmia hypertension and cerebral hemerrhage local anesthesia in end arteries-gangrene general anesthesia (digitalis)-ventricular fibrillation |
| Epistaxsis | نزيف الانف |
| Resuscitation | انعاش |
| gangrene | الغرغرينا |
| conjunctival blood vessels | اوعية داخل بياض العين |
| Noradernaline site of action | a1, weak on B1 , no B2 |
| Noradernaline routes of administration | IV infusion only |
| Noradernaline action CVS | blood vessels:VC of cutenous ,splanchic,renal blood vessels (a1)increases PR/blood pressure:increases (peripheral resistance) abolished after alpha blocker /heart:reflex bradycardia -vagal stimulation-bradycardia |
| theraputic uses of Noradernaline | used to elevate BP in hyposenststive states as in spinal anesthesia |
| side effects of Noradernaline | Hypertension , bradycardia , Headache |
| site of action of isoprenaline | on beta onnly |
| isoprenaline Routes of adminstration | SL-IV-inhalation |
| isoprenaline on CVS | heart:increase cardiac properties (B1) blood vessels :VD of coronary and skeletal BV (B2) Blood pressure:hypotension |
| isoprenaline on SMF | relexation of (eye, bronchi, GIT , urinary, uterus) |
| other actions of isoprenaline | acts on (liver -SK ms- fat cells) |
| theraputic uses of isoprenaline | heart block , bronchiak asthma |
| side effects of isoprenaline | Tachycardia,palpitation,arrhythmia general anaethesia - ventricular fibrillation |
| Tachycardia | سرعة ضربات القلب |
| palpation | رفرفة القلب |
| arrhythmia | لخبطة في ضربات القلب |
| Dopamine sites of action | dopaminergic receptors + B1+a |
| Dopamine routes of adminstration | IV infusion |
| Dopamine action with low dose | stimulate dopamine receptors (D1)causing VD of renal coronarty mesenteric and cerebral blood vessels |
| Dopamine action with moderate dose | stimulate b1 receptors-increase all cardiac properties and COP and systolic blood pressure |
| Dopamine action with high dose | stimulate alpha 1 receptors -VC of peripheral blood vessels and rise of diastolic BP |
| Dopamine theraputic effects | for different types of shock (cardiogenc,hemorrhagic,septic shock)- VD of renal blood vessels-inc renal blood flow Increase COP and systolic blood pressure Heart faliure and hypotension |
| side effects of Dopamine | Tachycardia,ventricular arrhythemia Nausea and vomiting |
| Dobutamine | selective B1+weak a |
| Dobutamine routes of adminstration | Iv infusion |
| Dobutamine action | stimulate B1 receptors - increase all cardiac properties (mainly contractility )and inc COP and systolic blood pressure |
| Dobutamine theraputic uses | For shock as it inc COP and systolic blood pressure for heart faliure and hypotension |
| Dobutamine side effects | tachycardia , ventricular arrhythemia |
| salmetrol , formetrol | non catecholamines long acting for bronchial asthma |
| terbutalin , salbutamol | non catecholamines intermedite acting on bronchial asthma |
| albuterol | non catecholamines short acting on bronchial asthma |
| phenylephirine , pseudoephedrine | non catecholamines old groups of nasal decongestant taken orally and locally |
| Naphazoline,Xylometazoline | non catecholamines Recent groups of nasal decongestant taken locally |
| methoxamine , midodrine , metraminol , phenyl ephrine (weaker than NA) | non catecholamines vassopressors |
| fenfluramine , phenmetrazine | non catecholamines anorexigenices |
| anorexigenices | فقدان الشهية |
| ephidrine and amphetamine | non catecholamines CNS stimulants |
| isoxsuprine , ritodrine | non catecholamines vassodilators and uterine relaxants |
| ephidrine site of actions | alpha and beta |
| ephidrine routes of administration | oral - injection repeated administration causes tolerance and tachyphylaxis |
| ephidrine action | as adrenaline but weaker (especially B)+no adrenaline reversal +cns actions :stimulate RC and VMC when depressed stimulate cerebral cortex and reticular formation -anxiety and insominia |
| adrenaline reversal | hypertension of adrenaline is reversed to hypotension after alpha blocker beacuse of vasodilation effects (b2) of adrenaline are unmasked - fall of BP |
| theraputic uses of ephidrine | adrenaline uses+nocturnal enuresis, narcolepsy, morphine toxicity , myathenia gravis (longer duration) |
| nocturnal enuresis | سلس البول |
| myathenia gravis | خلل في الSK MS |
| side effects of ephidrine | adrenaline +tolerance and tachyphylaxis retention of urine in male enlarged prostate CNS: insomina and anxiety |
| Amphetamine site of action | on alpha and beta |
| Amphetamine routes of adminstration | oral - injection |
| Amphetamine actions | as ephedrine + psychic :euphoria - alterness - delay fatique -anxiety -tremors-schizophrenia - convulsion analgesic:potentiate other analgesics affect feeding centres of hypothalmous inc RC , VMC -vasoconstriction /spinal:mono,polysynaptic reflexes |
| tremors | الارتعاش |
| euphoria | نشوة |
| convulsion | تشنجات |
| Amphetamine theraputic uses | (rarely used now)nocturnal enuresis ,narcolepsy ,obesity , hyperkinetic syndrome in children |
| nacrolepsy | خمول |
| hyperkinetic syndrome | فرط الحركة |
| side effects of Amphetamine | as ephidrine + anxiety -tremors-schizophrenia prolonged use : addiction |
| treatment of toxicity of Amphetamine | alpha blockers for hypertension dizepam for convulsion urine acidification by NH4CL - inc excretion |
| dizepam | مهدا للتشنجات |
| nasal decongestant routes of adminstration | oral - drops - spray |
| nasal decongestant theraputic uses | for common cold and rhinitis - sinusitis |
| rhinitis | التهاب الأنف |
| sinusitis | التهاب الجيوب الأنفية |
| nasal decongestant side effects | rebound congestion after stopping(iritant) long use - atrophy of cilia oily solution -inhaled-lipoid pneumonia prohibted for angina patients and hypertensive patients |
| nasal decongestant site of action | alpha 1 |
| vassodilators and uterine relaxants theraputic uses | vasodilators:in peripheral vascular diease uterine relaxants : contraction ring of uterus and premature labour |
| tyramine | present in cheese indirect in action and metabolized by MAO if patient took MAO inhibitor - hypertensive crises treated by a blockers |
| Sympatholytic Drugs | ( Sympathetic depressants)-Adrenergic receptor blockers-Adrenergic neuron blockers- Ganglion blockers-Centrally acting drugs |
| Adrenergic receptor blockers | α- blockers , β-blockers, α & β-blockers. |
| Adrenergic neuron blockers | which interfere with: -Noradrenaline release: guanethidine - Noradrenaline storage: reserpine. -Noradrenaline synthesis: α methyl dopa |
| Ganglion blockers | block transmission in ganglion as Trimethaphan |
| Centrally acting drugs | -α2-agonist (clonidine, guanafacine, guanabenz and α-methyl dopa). -Imidazoline receptors : Relimenidine |
| Beta blockers According to selectivity: | *Non selective :- Propranolol - Nadolol - Pindolol- Oxpernolol - Timolol (eye drops) Selective β blockers (block β1 > β2)- Atenolol - Metoprolol - Esmolol- Acebutolol - Celiprolol *β2 blockers: Butoxamine *α1 + β blockers: Labetalol - Carvediolol |
| Beta blockers According to solubility | Lipophilic:Well absorped oral Pass BBB-Hepatic metabolism Hydrophilic:Less absorbed-Not passBBB-Pass unchanged to urine |
| Propranolol-Metoprolol | lipophilic beta blockers |
| Atenolol- Nadolol | hydrophilic beta blockers |
| Propranol (Nonselective) actions on CVS | Heart:Dec all card prop, decmyocardial work and O2 requir-Antiarrythemic action: due to beta blocking effect- Na channelblocking – cell membrane stabilization-Bl.vessels: dec.blood flow to most of tissue.-Blood pressure:hypotension |
| hypotension | ( ↓ sympathetic flow- ↓ COP- ↓ renine relase –increase prostacyclin) |
| Propranol (Nonselective) action on SMF | Respiration: produce bronchospasm Eye:↓ IOP (Timolol) Metabolism:-↓ glucose: as it inhibit B in liver→ -- glcogenolysis → hypoglycemia -↓ renin - ↑ plasma k (hyperkalemia) |
| Theraputic uses of Propranol | Antianxiety.- Angina prophlaxis..- Acute myocardial infarction- Arrhythmias.-Hypertension ( 1ry / 2ry to pheochromocytoma with α blocker).-Glaucoma (by timolol).- Treatment of esophageal varices due to liver cirrhosis as it decreaseC.O.P-Thyrotoxicosis |
| - Angina prophlaxis | used in angina due to coronary atherosclerosis not due to spasm in coronary. |
| Side effects of Propranol | -Sedation –depression 2-Heart block 3-Cold extrimities-numbness-tingling 4-Hypotension 5-Bronchospasm 6-Hypoglycemia (in patient receive insulin or oral hypoglycemic drugs) 7-Hyperkalemia 8-Sudden discontinuation leads to sympathetic overactivity |
| Contraindications of Propranol | 1-Severe depression 2- Angina due to due to spasm in coronary(variant angina). 3-Bradycardia and heart block. 4-Peripheral vascular disease. 5-Hypotension 4 6-Bronchial asthma 7- Patient receive insulin or oral hypoglycemic drugs |
| -Intrinsic sympathetic activity (I.S.A) or partial agonistic activity | intial stimulation followed by block. prominent with pindolol and absent with propranolol . |
| α- blockers According to selectivity | |
| prazosin, trimazosin, tamsulosin, indoramin | Selective α1 blockers |
| yohimbine | Selective α2 blockers |
| ergotamine (partial agonist), , ergometrine, ergotoxin | -Ergot alkaloids: natural/ Non selective α blockers (block both α1 and α2). |
| dihydroergometrine | semi-synthetic -Ergot alkaloids Non selective α blockers (block both α1 and α2). |
| tolazoline, phentolamine | -Imidazoline derivatives -Ergot alkaloids Non selective α blockers (block both α1 and α2). |
| phenoxybenzamine- dibenamine | -β-Haloalkylamines -Ergot alkaloids Non selective α blockers (block both α1 and α2). |
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