pharm - pure & simple

8/20/2019 Pharm - Pure & Simple

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Pharmacology – Pure and Simple

Week 1 – Hypertension

Calcium Channel Blockers:Verapamil, Ni edepine, !mlodipine

• Blocks "#type Ca$% channels in tu'ules – reduced Ca$% intomyocyte and reduced mechanical activation of Ca$% releasechannels in S( – reduced myocyte contraction

• !rterial VS) – vasodilation – reduce BP• Heart – reduce H( and contractility Verapamil: higher a nity for heart• Nifedipine: higher a nity for VS)• SE: heart failure, hypotension, peripheral oedema, constipation

Potassium Channel *pener:)ino+idil, Pinacidil

*pens potassium channels in VSM – hyperpolarisation –rela ation ! vasodilation

Mino idil: Promotes hair gro"th – more o ygen to hair follicle –treats alopecia#

Pinacidil: $educes %lood pressure# SE: hypertrichosis &e cessive hair gro"th', tachycardia, angina#

Beta Blockers:!tenolol, Propranolol

!tenolol: Selecti e 'eta#1 'locker – %loc(s %eta!) receptors onheart – reduces cardiac output#SE: Bronchoconstriction &high dose %loc(s %eta!* as "ell',

inhi'its glycogenolysis - atigue./

Propranolol: Non#selecti e 'eta 'locker – %loc(s %eta!) and%eta!* – reduces cardiac output#SE: Bronchoconstriction , nightmares, depression, reducedglycogenolysis - atigue.

!lpha Blockers:Pra0osin

• !lpha#1 'locker – rela es VSM – reduces peripheral resistance#


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• SE: orthostatic hypotension , syncope , and nasal congestion #)i+ed !lpha Beta Blocker:"a'etolol

Selecti e alpha#1 + non#selecti e 'eta#1 and 'eta#$ 'locker –treats pregnancy induced pre#eclampsia/

• SE: orthostatic hypotension, a%rupt "ithdra"al arrhythmia, pre!eclampsia#

!C2 3nhi'itors:"isinopril, Captopril, 2nalapril

-nhi%its ./E – prevents .ngiotensin -- formation – reduces

vasoconstriction 0 aldosterone secretion – reduces peripheralresistance and %lood volume# SE: Cough -inhi'its 'radykinin 'reakdo4n. , 1rst dose

hypotension# -nteracts "ith potassium sparing diuretics – H5P2(6!"2)3!/

&hia0ide 7iuretics:Hydrochlorothia0ides

• 3nhi'its NaCl co#transporter in the distal tu'ule – reducessodium rea%sorption – increases sodium2potassium2chloridee cretion – reduce %lood volume – reduce %lood pressure#

• Blac( people respond %etter to thia3ides#• SE: hypokalemia , hyperuricemia -gout. , meta%olic al(alosis#

Potassium Sparing 7iuretics:Spironolactone, 2plerenone, !miloride, &riamterene

• Spironolactone 8 2plerenone: Block aldosterone receptor –increase sodium e cretion 0 decrease potassium e cretion –reduces %lood volume – reduces BPSE: hyperkalemia, gynecomastia , impotence#

• !miloride 8 &riamterene : Block sodium channel in distaltu'ule and collecting duct – inhi%its sodium rea%sorption andpotassium e cretion – reduce %lood volume#SE: hyperkalemia , heart palpitations, dry mouth, nausea2vomiting#

"oop 7iuretics:9urosemide

http://en.wikipedia.org/wiki/Orthostatic_hypotensionhttp://en.wikipedia.org/wiki/Faintinghttp://en.wikipedia.org/wiki/Nasal_congestionhttp://en.wikipedia.org/wiki/Faintinghttp://en.wikipedia.org/wiki/Nasal_congestionhttp://en.wikipedia.org/wiki/Orthostatic_hypotension


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• 3nhi'its Na 6 $Cl co#transporter in &!" o loop o henle –%loc(s Na/l rea%sorption – reduces %lood volume#

• SE: meta'olic alkalosis, hypokalemia , hyperuricemia ,hypomagnesemia

!ngiotensin 33 inhi'itors:"osartan, Valsartan

• Block !33 receptors ! on VSM and adrenal corte &%loc(saldosterone release'#

(enin inhi'itors:!liskiren

Blocks renin – prevents activation of renin angiotensin aldosterone

system

"3P37 "*W2(3N 7(; S:

Statins:!tor astatin, 9lu astatin

3nhi'it H) #Co! reductase – inhi'it cholesterol synthesis inliver – stimulate increase in "7" receptors on hepatocytes –

increase "7" uptake in liver – increase "7" cata'olism – reduceplasma cholesterol – reduce atherosclerosis .lso, decrease triglycerides + increases plasma H7" +

maintain pla


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"i er uses cholesterol to produce 'ile acids ! se4uestrantsadsor's 'ile acids !reduces 3 a'sorption + increasedcholesterol e+cretion ! reduced plasma cholesterol !stimulates the liver to produce more 'ile acids ! uses more

cholesterol – further drop in cholesterol – reduced atherosclerosis SE: 5- disorders

Week $ # Heart 9ailure

!nticoagulants:Heparin ")WH

• Binds !ntithrom'in 333 – increases its activity %y )666!fold –inacti ates 9actor >a % throm'in – reduced clot formation#

• ")WH only inacti ates 9actor >a , it also has a longer half life#• 7sed for: V&2, P2, atrial ='rillation, H9 #• SE: haemorrhage, throm'ocytopenia &reduced platelets'#

War arin

• 3nhi'its itamin 6 epo+ide reductase – prevents vitamin 8dependant car%o ylation of glutamate residues of 9actor 33, V33, 3>and > #

• 7sed for: same as heparin 0 prosthetic heart al ethrom'oem'olism #

Monitored "ith 3N( -prothrom'in time. – usually $ to ?/• SE: haemorrhage, teratogen , a%normal %one development#

Cardiac Stimulant:7igo+in

• 9igitalis glycoside – inhi'its Na 6 pump – increasesintracellular sodium – slo4s the e+trusion o calcium ia

Na Ca e+change transporter – increases intracellular calcium– increases contractility o heart – slo4s atrio entricular


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conduction – increases atrioventricular period – decreases heartrate/

• 7sed for: ! =', heart ailure #• SE: arrythmias , yello4 'lurred ision , nausea2vomiting#

Week ? – (heumatic Heart 7isease!nti#muscarinic:!tropine

• Bloc(s %inding of ./h to muscarinic receptors – 'locksparasympathetic - agal. activity – increases heart rate#

• 5iven as a treatment for S";7 2&salivation , lacrimation , urination , diaphoresis , gastrointestinal motility, emesis '

• Pre ents 'radycardia during surgery , used as mydriatic , forincontinence#

• SE: tachycardia, mydriasis &pupil dilation', delirium, dry mouth,constipation#

Beta#"actams:Penicillin!mo+icillin % Cla ulonate -!ugmentin.

• !mo+icillin: -nhi%its cross#linking o cell 4all peptidoglycans –preventing formation of %acterial cell "all + Cla ulonic acid: -nhi%its 'eta lactamase

• streptococci &$ 9 – 5roup .' , pneumococci, meningococci, syphilis• Penicillin V -Pheno+ymethylpenicillin. ! tonsillitis, pharyngitis,

rheumatic fever, s(in infections• Penicillin -Ben0ylpenicillin. ! pneumonia &community

ac4uired', endocarditis, gonnorrhea, cellulitis, meningitis ! more

active against 5ram Negative

http://en.wikipedia.org/wiki/Salivationhttp://en.wikipedia.org/wiki/Lacrimationhttp://en.wikipedia.org/wiki/Urinationhttp://en.wikipedia.org/wiki/Diaphoresishttp://en.wikipedia.org/wiki/Gastrointestinalhttp://en.wikipedia.org/wiki/Emesishttp://en.wikipedia.org/wiki/Salivationhttp://en.wikipedia.org/wiki/Lacrimationhttp://en.wikipedia.org/wiki/Urinationhttp://en.wikipedia.org/wiki/Diaphoresishttp://en.wikipedia.org/wiki/Gastrointestinalhttp://en.wikipedia.org/wiki/Emesis


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• SE: 5- pro%lems, allergic reactions -rashes, anaphylacticshock, sei0ures. , diarrhoea, super infection#

Cephalosporins

Ce uro+ime• -nhi%its cross#linking o cell 4all peptidoglycans – preventing

formation of %acterial cell "all• (esistant to many 'eta#lactamases• ;or( %etter than penicillins on many gram negatives• 5ram Negative: enterobacter, citrobacter • SE: 5- pro%lems, rash, diarrhoea, super infection

Week @ – !sthma

(2"32V2(S:

Beta !gonists:Short acting # Sal'utamol -!l'uterol., &er'utaline"ong acting # Salmeterol, 9ormoterol

• !cti ates Beta#$ receptors in %ronchial SM – increases c!)P –activates protein (inase . – inhi'its myosin phosphorylation –muscle rela+ation – %ronchodilation#

• .lso ! increases cilia 'eating 0 'locks agal impulses &decrease SM constriction'#

• SE: tachycardia, muscle tremor , restlessness#

)ethyl+anthines:&heophylline, !minophylline

• 3nhi'its phosphorylation o phosphodiesterases – pre entscon ersion o c!)P to !)P – increase in c.MP ! activates protein(inase . – inhi%its myosin phosphorylation – muscle rela ation –%ronchodilation#

• .lso acti ates histone deacetylase – do4nregulates

e+pression o pro#inAammatory genes – reduced & cellproli eration and cyto(ine production#


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• SE: tachycardia, nausea2vomiting, insomnia#

!nti#)uscarinic:

3pratropium, &iotropium

• Blocks muscarinic receptors in 'ronchial S) 0 reduceshistamine stimulation o 'ronchial agal a erents ! preventsvagal stimulated %ronchoconstriction – %ronchodilation#

• SE: cough, nasal dryness#

P(2V2N&2(S:

Corticosteroids:Beclamethasone -inhalation., Prednisolone -oral.

• 9i infections, muscle"asting, osteoporosis, psychosis, dia'etes , hypertension ,hypokalemia , s(in atrophy, poor "ound healing, gro4thsuppression in children , /ushingoid appearance &moon face,%u


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"eukotriene synthesis inhi'itor:ileuton

•

3nhi'its D#lipo+ygenase – inhi'its leukotriene synthesis –pre ents 'ronchconstriction, mucous hypersecretion, air4ayinAammation, oedema/

• SE: hepatitis &increased aminotransferase levels', =u!li(e syndrome,dyspepsia#

)ast Cell Sta'ilisers:Cromolyn, Nedocromil

•

Blocks calcium entry into mast cells and 'asophils – pre entsrelease o histamine , leu(otrienes, other mediators#• SE: nasal and throat irritation#

3g2 antagonist:*mali0uma'

• Binds to 3g2 anti'ody – pre ents 'inding o 3g2 to mast cellsand 'asophils – %loc(s release of histamine and leu(otrienes#

• SE: anaphyla+is - severe allergic reaction'#

!S&H)! 73! N*S3S:

Challenge &ests # Bronchoconstrictors

)ethacholine ! muscarinic agonist! imitates acetylcholine! used to

diagnose asthma

Histamine ! stimulates vagal a


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Week E – laucoma

F !G;2*;S H;)*( S2C(2&3*N:

Car'onic !nhydrase 3nhi'itor:!ceta0olamide, 7or0olamide

• .cts on ciliary 'ody epithelium in the posterior cham%er of eye –inhi'its car'onic anhydrase ! inhi'its 'icar'onate synthesis –reduces sodium transport -'icar' sodium co#transporter. –

reduced a


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!G;2*;S H;)*( *;&9"*W:

Prostaglandin#9$ analogues:"atanoprost

•

Passes through cornea 'inding prostaglandin 9P receptor !acti ates matri+ metalloproteinases – reduces outAo4resistance – increases a


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Week J – 2pilepsy

Sodium Channel Blockers:Phenytoin, Car'ama0apine, "amotrigine

• Blocks oltage gated Na% channels – preferentially 'locks cells=ring 4ith high re


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Blocks oltage gated Na% channels > 3ncreases !B! 'yincreasing release decreasing meta'olism reducingreuptake > Blocks type calcium channels – 'locks ? sec=ring rhythm in thalamic neurons &characteristic of a'sence

sei0ures ' 7sed for: a%sence sei3ures, comple partial sei3ures, tonic clonic,

myoclonic, migraines, %ipolar# SE: 5- pro%lems, di33iness, hepatoto icity, sedation, teratogen

Sodium Channel Blockers !B! augmenter lutamate (eceptorBlocker:

&opiramate

Blocks oltage gated Na% channels > 3ncreases stimulation o !B! ! receptors >Blocks glutamate -!)P!. receptor #

7sed for: partial sei3ures, tonic clonic sei3ures# SE: ata ia, fatigue, impaired concentration 0 memory, speechpro%lems, diplopia#

Bar'iturates:

Pheno'ar'ital

Stimulates !B! ! chloride channels – increases duration ofchloride ion channel opening> .lso inhi'its glutamate acti ationat the !)P! receptor/

• 7sed for: e'rile sei0ures in children/• SE: delirium, dependence, hangover, lethargy#

Ben0odia0apenes:

Short acting # )ida0olam, !lpra0olam, "ora0epam, Clona0epam"ong acting # 7ia0epam, Chlordia0epo+ide -"i'rium.

Stimulates !B! ! chloride channels – increases re


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SE: dependence -short acting. , dro"siness, amnesia, respiratorydepression#

Withdra4als: an+iety, insomnia, irrita'ility, depressed mood/ * erdose: 9luma0enil – competiti e inhi'itor of the 'en0o

'inding site on !B! ! /

*thers:a'apentin, Prega'alin: !B! analog ! does not act on 5.B.

receptor – may stop e pression of /a*+ channels

9el'amate: Blocks N)7! receptors

#drugs: olpidem, opiclone: Non#'en0odia0epine hypnotics #Binds !B! ! at same location as %en3os# "ess dependence + 'ettersleep -lose less (2) sleep./

Week K – )ultiple Sclerosis

Ben0odia0apenes:

Short acting # )ida0olam, !lpra0olam, "ora0epam, Clona0epam"ong acting # 7ia0epam, Chlordia0epo+ide -"i'rium.


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Stimulates !B! ! chloride channels – increases re


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Beclamethasone -inhalation., Prednisolone -oral.

• 9i infections, muscle"asting, osteoporosis, psychosis, dia'etes , hypertension ,hypokalemia , s(in atrophy, poor "ound healing, gro4thsuppression in children , /ushingoid appearance &moon face,%u


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&hiorida0ine: (etinal pigmentation -melanosis. Haloperidol: "o4er muscarinic # High 2PS2s

!N&3PS5CH*&3CS – S2C*N7 2N2(!&3*N – !&5P3C!"

!typical: "ess 2PS2sClo0apine

Blocks 7@ M 7$ -"ess 2PS2s. >Blocks )1#)D -less 2PS2s. Blocks DH&$a -anti hallucinations, less

2PS2s. >Blocks DH&$c -4eight gain./• SE: ! (!N;"*C5&*S3S , plus all a%ove#

*lan0apine, (isperidone

Blocks DH&$ M 7$ Blocks )1 Blocks H1• SE: 4eight gain , type * dia%etes, orthostatic hypotension, plus all

a%ove#


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Week 11 – !n+iety 7ementia

!cetylcholinesterase inhi'itor:Physostigmine, 7onepe0il, alantamine

3nhi'its acetylcholinesterase – decrease %rea(do"n of ./h –increase synaptic .ch – slo4s decline o cogniti e unction/

• 7sed for dementia, .l3heimers#• SE: cholinergic syndrome &overdose', 5- pro%lems, nausea2vomiting,

%radycardia#

(i astigmine

• 3nhi'its acetylcholinesterase and 'utrylcholinesterase-decreased 'reakdo4n o succinylcholine. – rest same asa%ove#

• Meta%olised at site of action – no interactions#

lutamate antagonist:)emantine

• @o" a nity, non!competitive, N)7! receptor antagonist –prevents e+citoto+ic glutamate e ects – decreases neuronalloss – slo4s decline o cogniti e unction #

• SE: confusion, insomnia, headache#

!n+iolytic:Buspirone

• !cti ates presynaptic DH&1a -inhi'itory neurotransmission. in dorsal raphe nucleus – decreases =ring o serotonergicneurons #

7sed for: generalised an+iety disorder - !7.• SE: headache, fatigue, %lurred vision, s"eating, tachycardia#


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Bar'iturates:Pheno'ar'ital

Stimulates !B! ! chloride channels – increases duration ofchloride ion channel opening> .lso inhi'its glutamate acti ationat the !)P! receptor/

• 7sed for: e'rile sei0ures in children/• SE: delirium, dependence, hangover, lethargy#

Ben0odia0apenes:

Short acting # )ida0olam, !lpra0olam, "ora0epam, Clona0epam"ong acting # 7ia0epam, Chlordia0epo+ide

Stimulates !B! ! Cl# channels – increases re


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Week 1$ – 2ating 7isorder

Canna'inoid agonist:7rona'inol

• CB#1 rcp agonist – increases appetite #• 7sed for anore+ia• SE: short term memory

Canna'inoid antagonist:(imona'ant

CB1 rcp antagonist – suppresses appetite # 7sed for anti#o'esity, smo(ing cessation, %loc(s canna%is e


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Week 1? – !cute (enal 9ailure

Beta Blockers:Propranolol

Non#selecti e 'eta 'locker – %loc(s %eta!) and %eta!* – reducescardiac output#SE: Bronchoconstriction , nightmares, mood depression, inhi'itsglycogenolysis - atigue.

Nasal Sinus 7econgestant:Pseudoephedrine

!lpha adrenergic receptor agonist 0 increases release o N! – vasoconstriction and cardiac stimulation#

SE: nervousness, tachycardia, insomnia, /NS stimulation#

;rologic !gent:&era0osin

Selecti e alpha#1 receptor antagonist – lo"ers BP – decreasesoutAo4 o'struction caused %y an enlarged prostate #

SE: irst dose syncope, priapism, erectile dysfunction#

&ype 1 (enal &u'ular !cidosis:

"ithium, !mphotericin B


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• 9ailure o H% secretion %y the (idneys#

&ype $ (enal &u'ular !cidosis:!ceta0olamide

• 9ailure o HC*?# rea'sorption %y the (idneys ! car%onicanhydrase inhi%itor

Week J – Pneumonia

P(*&23N S5N&H2S3S 3NH3B3&*(S:

)acrolides 2rythromycin, !0ithromycin, Clarithromycin

• Binds to DLS su'unit ! ! pre ents peptidyltrans erase addingpeptidyl to !!s ! inhi%its protein synthesis#

Bacteriostatic• 5ram Positive: streptococcus pneumonia, pneumococci,

staphylococci, enterrococci.• 5ram Negative: Chlamydia, haemophilus infuenza , legionella• ; % "(&3s &phanyngitis, pneumonia' + sinusitis, otitis media• SE: 5- pro%lems

&etracyclines7o+ycycline

• Bind to ?LS su'unit ! pre ents 'inding o aminoacyl#t(N! tori'osome su'unit – inhi%its protein synthesis#

Bacteriostatic• 5ram Negative: Chlamydia, gonorrhoea, syphilis, Borrelia

burgdor eri (Lyme Disease) mycoplasma, Ric ettsia,• S&3s , acne, cholera• SE: permanent teeth discolouration , teratogen ,

photosensitivity, 5- pro%lems

!minoglycosides:


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entamicin, Streptomycin

• Binds ?Ls su'unit – misreading of genetic code – inhi%its proteinsynthesis#

•

Bacteriocidal

7N! S5N&H2S3S 3NH3B3&*(S:

9luoro


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Binds to the 7#alanyl#d#alanine portions o peptidoglycan !prevents cross#linking o d#alanine and pentaglycine chain –prevents cell "all synthesis

7sed for: )(S! &methicillin resistant staphylococcus aureus'#

!N&3 P(*&! *!":

Nitroimada0ole:)etronida0ole

• Produces ree radicals that attack 7N! and proteins• 7sed for !N!2(*B3C B!C&2(3! : Clostridium di!cile,

trichomoniasis ("aginitis)

*&H2(S:

!nti#&u'erculin:(i ampicin

• 3nhi'its (N! polymerase – prevents transcription to (N! andtranslation to proteins

• Mycobacterium -eg/ &u'erculosis. – sometimes used asprophyla is for #eisseria meningitidis &meningococcal ' infection

Sul onamide:Sul adia0ine

• 3nhi'its olic acid synthesis – %loc(s %acterial 9N. synthesis 7sed for: to+oplasmosis, ;&3s

!N&3#B3*&3C (2S3S&!NC2:

! Betalactamase ! %rea(s do"n B!lactam ring &gram!neg'

! Plasmid ! transfer of genetic info onto other %acteria

! Penicillin 'inding proteins ! change shape! cannot %ind

! Porins ! conformation change! .Bs cannot enter %acteria

http://en.wikipedia.org/wiki/Meningococcalhttp://en.wikipedia.org/wiki/Meningococcal


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Week 1L – )ultiple )yeloma

NS!37s:!spirin -acetylsalicylic acid.

•

.dds acetyl group to /?D – irre ersi'ly inhi'its C*>#1 – preventsconversion of arachadonic acid to P H$ &analgesic, anti!pyretic,anti!in=ammatory e#$ -less pre erentially.

SE: 3 'leeding, heart 'urn , renal ailure

7iclo enac, 3'upro en

•

Non#selecti e, re ersi'le C*> inhi'itor ! prevents conversion of arachadonic acid to P H$ &analgesic, anti!pyretic, anti!in=ammatory e#? inhi'itor ! prevents conversion of arachadonicacid to P H$ &analgesic, anti!pyretic'

SE: epatic failure &overdose'


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* erdose: lutathione ! conIugates to N!PG3 and helps todeto ify it ! "hen normal path"ay saturated -i/e/ all glutathionehas 'een spent. , accumulated N!PG3 reacts 4ith hepaticen0ymes , killing hepatocytes ! treatment for ?9 is N#!cetyl#"#

Cysteine ! augments glutathione reser es in %ody – protectshepatocytes from N.P -

*pioids:Codeine

C5P@DL$7O cataly0es codeine to morphine ! activates u opioidreceptors ! opens 6% channels and closes Ca$%channels ! decreases release of SP and other N&s – inhi'its pain

neurotransmission in CNS SE: respiratory depression, addiction

"ocal !naesthetic:"idocaine, Procaine

Blocks oltage gated Na% channels – %loc(s nerve conduction!reduced sensation

SE: di33iness, dro"siness, confusionChemotherapeutic !gent:Vincristine

%inds to tu'ulin dimers – inhi'its assem'ly o mitotic spindlemicrotu'ules – halts mitosis in metaphase – prevents celldivision and tumour gro"th

SE: alopecia &hair loss', peripheral neuropathy, constipation,hyponatremia

Cisplatin

Platinum compound ! cross links 7N! strands – interferes "ithmitosis

SE: nausea, vomiting & highly emetogenic – use "ith ondansetron# anti#emetic ' nephroto icity, neuroto icity

)ethotre+ate

3nhi'its olate reductase – prevents formation of folate – stops9N. %ase production– halts mitosis in S phase

http://en.wikipedia.org/wiki/Acetylcysteinehttp://en.wikipedia.org/wiki/Acetylcysteinehttp://en.wikipedia.org/wiki/Acetylcysteinehttp://en.wikipedia.org/wiki/Acetylcysteine


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7sed for cancer, $., psoriasis SE: teratogenic , ulcerative stomatitis &in=ammation of mucous

lining of mouth', leu(openia, throm%ocytopenia, anaemia

Week 1$ – Herpes Simple+ Virus

Nucleoside !nalogues:!ciclo ir, anciclo ir

Nucleoside analogues incorporated into iral 7N! ! inhi%itsiral 7N! polymerase – causes iral 7N! chain termination

7sed for: HSV#1 &trigeminal', HSV#$ &sacral root ganglion', V V &chic(en po ', 2BV &glandular fever', C)V &salivary glands'

SE: di33iness, diarrhoea, nausea


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Guick 7rugs*steoporosis:

2tidronate: ) st generation %isphosphonate ! 'inds to hydro+ypatitecrystals in %ones ! reduces osteoclastic acti ity + decreasedacti ity o osteo'lasts – reduces %one resorption !

!lendronate and (isedronate : * nd generation %isphosphonate – 'indsto hydro+ypatite crystals in %ones ! reduces osteoclastic acti ity !doesn t inhi'it osteo'lasts FSE: *esophagitis

)yasthenia ra is:Botulinum &o+in ! clea es SN!(2 proteins ! %loc(s fusion of esicles4ith neuronal mem'rane ! no release of !Ch ! %loc(s neuromusculartransmission – relieves spasticity

7antrolene ! inhi'its ryanodine receptor ! reduced intracellularcalcium from S$! relieves spasticity


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Neostigmine ! acetylcholinesterase inhi'itor – medium acting &)!*hrs' – S2: 'radycardia2drophonium -&ensilon. ! acetylcholinesterase inhi'itor – shortacting ! &)6mins'

C*P7:Varenicline# acts on nicotinic receptors in Ventral &egmental !rea !'locks pleasura'le e ects o nicotine ! also stimulates dopaminergicneurons in nucleus accum'ens ! stimulates release o dopamine !increases risk o addiction

)3:Clopidogrel ! 'locks platelet P$5 receptor ! prevents stimulation %y!7P ! prevent platelet aggregation

&N ! 5lyceryl Crinitrate! forms nitric o+ide ! increased c )P !vasodilation – S2: headache

"o4 dose ! en M art dilation ! less venous return ! decreasedcontractility -9rank#Starling.

High dose ! art M en dilation ! decreased CP$ ! decreased coronaryartery spasm

Su'lingual– enters venous circulation &%y!pass 1rst pass'– aster and less risk o en0yme degradation ! stomach and %ile

3(7S:*+ytocin ! %inds to o+ytocin receptor ! activation of phospholipase C ! increased intracellular Ca$% ! activation of )"C6# ;&2(3N2

C*N&(!C&3*N

&*C*"5&3CS!tosi'an ! o+ytocin receptor 'locker(itrodine, &er'utaline ! 'eta $ agonist ! uterine muscle rela ation&tocolytic'3ndometacin ! C*> inhi'itor ! no prostaglandins – SE: renaldys unction, delayed closure o ductus arteriosus)agnesium sul ate ! 'locks inAu+ o Ca$% into myometrial cells

*(7:


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Cimetidine, (anitidine, 9amotidine - antac. ! H$ receptorantagonists ! prevent activation of parietal cell H% 6% !&Pase –reduced acid secretion – SE: Pernicous !naemia -)egalo'lastic. ! dueto reduced release o intrinsic actor &needed for Vit B1$ a'sorption

!folate regeneration' from parietal cells

*mepra0ole, "ansopra0ole – proton pump inhi'itors ! irreversi%lyinhi'it H% 6% !&Pase proton pump in gastric parietal cells ! noreduction in release of -ntrinsic factorNB : con erted to acti e orm in acidic en ironment ! antacids caninterfere

)isoprostal ! synthetic prostaglandin 21 analogue ! decreased acid,increased mucus ! la%our induction and erectile dysfunction

)etoclopramide ! antiemetic and gastropro(inetic! 7$ antagonist +H@ antagonist ! increased tone o contractions and rela+essphincters ! increased gastric emptying

7ia'etes:lucagon -!lpha cells. ! adenylyl cyclase! increased c.MP!

glycogenolysis % gluconeogensis – inGection to treat se erehypoglycemia# 7ia'etic coma

3nsulin -Beta cells. ! ";& $ transporter ! ta(es up glucose ! increase!&P ! closes potassium channel ! depolari0es 3slet cells – insulinreleased

Sul onylureas ! acts on 'eta cells o pancreas# 'locks !&P sensiti e6% channels ! depolari0es %eta cell! Ca$% inAu+ ! insulin release !7) 33

)et ormin – Biguanide ! decreased glucose release rom

hepatocytes + increased uptake o glucose into adipocytes 8muscle cells ia ";&@ – 7) 33 SE: lactic acidosis

3ncretins ! "P &5lucagon!li(e peptide )' and 3P &glucose dependentinsulinotropic polypeptide' ! increase insulin secreted from %eta cells(heumatoid !rthritis:"eAunomide ! inhi'its pyrimidine synthesis in acti ated & cells –reduced in=ammation


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Sul asala0ine ! con erted to D#aminosalicyclic acid %y 'acteria incolon ! H!aminoalicyclic acid! ree radical sca enger – reducedin=ammation

2tanercept, 3nAi+ima' ! &N9 alpha antagonists – pre entupregulation o ='ro'lasts % osteoclasts "hich produce ))Ps thaterode cartilage and 'one

!nakinra ! 3"#1 antagonist ! pre ents upregulation o ='ro'lasts %osteoclasts "hich produce ))Ps that erode cartilage and 'one

)ethotre+ate – olic acid antagonist – prevents 9N. %ase synthesis –often used in com%ination "ith Etanercept

(itu+ima' ! monoclonal anti'ody against C7$L -B lymphocytes.

Shoulder 7islocation:"e o'upi acaine – interscalene 'lock ! peripheral nerve %loc( of'rachial ple+us – %et"een anterior 8 middle scalene

Cere'ral Palsy:Clonidine, &i0amidine ! alpha $ agonist ! reduce toneNB: Clonidine I BP &reduce /? 0 PV$', &i0amidine I muscle rela+an t&reduce spasms'

Parkinson s 7isease:(opinirole, Bromocriptine – 7$, 7? agonist ! inhi%its indirectpath4ay ! decreased termination of movement

"#dopa, Car'idopa ! precursor of dopamine ! "#7*P! can cross BBB ,dopamine canAt –normally synthesi0ed rom "#tyrosine and con ertedto dopamine in CNS 'y decar'o+ylase en0yme – also con erted in

PNS %y same en3yme, therefore, car'idopa -PNS 7ecar'o+ylase3nhi'itor. used 4ith "#7opa as it can %e acti e in the PNS %utcannot penetrate into the CNS allo"ing dopamine to orm only inCNS

2ntacapone ! inhi'its C*)& – prevents conversion of "#7*P! to ?#o#methyldopa "hich cannot cross BBB ! li(e car%idopa, it can also %e usedas adIunct to "#7*P!

http://en.wikipedia.org/wiki/Biosynthesishttp://en.wikipedia.org/wiki/L-tyrosinehttp://en.wikipedia.org/wiki/Biosynthesishttp://en.wikipedia.org/wiki/L-tyrosine


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Selegiline ! inhi'its )!*#B – prevents 'reakdo4n o dopamine – may%e used 4ith "#dopa , ho"ever, there is an increased risk o an acutehypertensi e episode !

Headache )igraine:Car'ama0epine, Phenytoin - Blocks oltage gated Na% channels –preferentially 'locks cells =ring 4ith high re


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after release into synapse

Bipolar ! decreased N. ! decreased )HP in urine & N! meta'olite '!n+iety – increased N. – increased )HP in urine – associated "ith

unipolar depressionSuicide Victims ! Brain and /S ! decreased D#H3!! &meta%olite ofSerotonin '

7e+amethasone suppression test ! glucocorticoid ! should suppress/$ , ./C ! no e

pharm - pure & simple

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