curs-nr-4 g gjj

7/24/2019 Curs-nr-4 g gjj

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Georgeta erban Substane medicamentoase cu aciune asupra SNV

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SUBSTANE MEDICAMENTOASE SIMPATOLITICE

A. ALFA-ADRENOLITICE

I. -ADRENOLITICE NATURALE

I.1. ERGOALCALOIZI (ALCALOIZII CORNULUI SECAREI) I DERIVAII LOR

- ergoalcaloizi cu structur polipeptidic: ergotamina, ergosina, ergotoxina i derivaii lor.

HN

NCH3

H

CO NH

N

ON

O O

R1

2

56

789

10

2'

5'

8'

12'

OH

R2

Ergotamina R1= R2= CH2C6H5CH3Ergosina R1= CH3

Ergocristina R1= CH(CH3)2 R2= CH2C6H5

Ergocriptina R1= CH(CH3)2 R2= CH2CH(CH3)2

Ergocriptina R1= CH(CH3)2 R2= CHCH2CH3

CH3Ergocornina R1= CH(CH3)2 R2= CH(CH3)2

R2= CH2CH(CH3)2

- ergoalcaloizi cu structur amidic: ergometrina, metilergometrina, metisergida, lisergida

(LSD).

HN

NCH3

H

CO NH CHCH2OH

CH3

Ergometrina

NICERGOLINA BROMOCRIPTINA MESILAT

N

NCH3

H5

6

789

H3C

H3CO

CH2OCO

N

Br

HN

NCH3

H

N

ON

O O

CH

2

56

789

10

2'

5'

8'

12'

OH

CH2CH(CH3)2

H3C CH3

CH3SO3H.CONH

Br


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METILERGOMETRINA MALEAT LISERGIDA

HN

NCH3

H

CO NH CHCH2OH

CH2CH3

CH

COOHCH

COOH

HN

NCH3

H

CO N

CH2CH3

CH2CH3

I.2. YOHIMBINA

NH

N1 311

6

14

16 18

20

H3COOC

H

H OH

II. -ADRENOLITICE DE SINTEZ

II.1. -HALOALCHILAMINE

FENOXIBENZAMINA CLORHIDRAT

NCH2CH2Cl

OCH2CH

CH2

CH3

. HCl

II.2. DERIVAI DE IMIDAZOLIN

TOLAZOLINA CLORHIDRAT FENTOLAMINA MESILAT

ClNH

NH

CH2

.NH

N

CH2

CH3SO3H

N CH3

HO

II.3. DERIVAI DE CHINAZOLIN

PRAZOSIN

N

N

NH2

N

H3CO

H3CO N C

O

. HCl

O

NCH2CH2Cl

R

R


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TERAZOSIN

N

N

NH2

N

H3CO

H3CO N C

O

. HClO

. 2H2O

DOXAZOSIN

N

N

NH2

N

H3CO

H3CO N C

O

. CH3SO3HO

O

TRIMAZOSIN

N

N

NH2

N

H3CO

H3CO N COOCH2

OCH3

C CH3

CH3

OH

. HCl

BUNAZOSIN

. HClN

N

NH2

N

H3CO

H3CO N COCH2CH2CH3

ALFUZOSIN

N

N

NH2

N(CH2)3NHCO

H3CO

H3CO

CH3

O

B. SIMPATOLITICE CENTRALE: SIMPATOLITICE AGONITI ALPHA 2-ADRENERGICI PRESINAPTICII/SAU I1-IMIDAZOLICI(ANTIHIPERTENSIVE CENTRALE)

CLONIDINA MOXONIDINA GUANFACINA

Cl

Cl

N

NH

HN

N

N

Cl

HN

NH

N

H3C

OCH3

Cl

Cl

CH2CONH-C-NH2

NH


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GUANABENZ ACETAT RILMENIDINA FOSFATCl

Cl

CH N NH C NH2

NH

. CH3COOH

CHN

O

HN. H3PO4

METILDOPA

CH2HO

HO

C

NH2

COOH

CH3

. 1,5H2O

C. NEUROSIMPATOLITICE

TOSILAT DE BRETILIU GUANETIDINA SULFAT

CH2

Br

N

CH3

CH3

H3C SO3C2H5

N

H

CH2CH2 N C NH2NH2H

2

SO42-

REZERPINA

NH

NH3CO

H

H3COOC OC

H

H

OCH3

OCH3

OCH3

OCH3

O

1 311

6

14

16 18

20

D. BETA-ADRENOLITICE (BLOCANTE -ADRENERGICE, -BLOCANTE)

I. DERIVAI DE DICLORIZOPRENALIN

II. DERIVAI DE ARILOXIPROPANOLAMIN

Ar-O-CH2CHCH2NH R

OH

CH3SO2NH CHCH2NHCH(CH3)2

OH

Sotalol

HO

H2NOC

CHCH2NHCH

CH3

CH2CH2

LabetalolOH


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BETA-BLOCANTE

FORME FARMACEUTICE, SPECIALITI1. ATENOLOL - acioneaz predominant 1-blocantInd: HTA, angin pectoral, aritmii cardiace, infarct miocardic (IM)Spec: ATENOLOL cp 50 mg, cp filmate 50 mg, 100 mg

ATENOCOR cp 50 mg, 100 mg

ATECOR cp 100 mg, BLOCOTENOL cp 50 mg, 100 mgHYPOTEN cp film 50 mg, 100 mg, VASCOTEN cp film 100 mg.

2. METOPROLOL - acioneaz predominant 1-blocant (2-blocant doar la doze mari)Ind:- HTA, profilaxia crizelor de angin pectoral

- IMA (infarct miocardic acut)- aritmii supraventriculare (tahicardie, flutter atrial)- aritmii ventriculare (extrasistole ventriculare, tahicardie ventricular)

Spec: BETALOC sol inj 1 mg/ml, cp retard 25 mg, 50 mg, 100 mgBETAPROL cp 50 mg, 100 mgBLOXAN cp 100 mgMETOPROLOL cp, VASOCARDIN cp, VASOCARDIN SR 200 cp eliberare

prelungit

3. TALINOLOL - acioneaz predominant 1-blocantInd: HTA, boal cardiac ischemic, IMA, aritmii cardiaceSpec: CORDANUM dj 50 mg (folosit frecvent ca antihipertensiv)

4. CELIPROLOL - 1-blocant selectivInd: - HTA n monoterapie sau n asociere cu alte antihipertensive

-profilaxia crizelor de angin pectoralSpec: CELIPRES, CELIPROL

5. BISOPROLOL - 1-blocant selectiv

Ind: HTA n monoterapie sau n asociere cu alte antihipertensiveSpec: BISOGAMMA, BISOMERCK cp filmate 5 mg, 10 mg

BYOL cp film 5 mg, 10 mgCONCOR cp film 2,5 mg, 5 mg, 10 mg

6. BETAXOLOL - 1-blocant selectivInd: - admin intern n HTA monoterapie sau terapie combinat cu alte antiHTA

- admin local conjunctival glaucom cronic, hipertensiune intraocularSpec: BETAC, LOKREN cp film 20 mg

BETAXOLOL, BETOPTIC, OPTIPRES sol oft 0,5%BETOPTIC S susp oft 0,25%

7. CARTEOLOL - -blocant neselectivInd: - glaucom, hipertensiune intraocular (antiglaucomatos)Spec: CARTEOL sol oft 1%, 2%

8. METIPRANOLOL- -blocant neselectivInd:- angin pectoral, stri postinfarct, aritmii cardiace, HTASpec:TRIMEPRANOL cp 10 mg

9. PROPRANOLOL - -blocant neselectivInd:- angin pectoral, aritmii cardiace


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- HTA monoterapie, terapie combinat- profilaxia migrenelor

Spec:PROPRANOLOL cp 10 mg, 40 mg

10. TIMOLOL- -blocant neselectiv- reduce tensiunea intraocular glaucom, hipertensiune ocularSpec: ARUTIMOL, OPHTAMOLOL, TIMO-GAL, TIMOLOL, TIMOPTIC sol oft 0,5%

NYOLOL gel oft 0,1%

11. NEBIVOLOL- 1-blocant selectiv- stimuleaz eliberarea de oxid nitric (efect vasodilatator)

Ind: - HTASpec:NEBILET cp 5 mg

curs-nr-4 g gjj

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